Search Result
Results for "
efflux
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-112505
-
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BCRP
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Cancer
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Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively .
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- HY-P2576
-
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Bacterial
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Infection
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Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K + efflux and inhibits cell viability with EC50 of 5 μM .
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-
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- HY-149811
-
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Bacterial
Parasite
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Infection
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Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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- HY-149812
-
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Bacterial
Parasite
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Infection
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Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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-
-
- HY-149810
-
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Bacterial
Parasite
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Infection
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AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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-
-
- HY-Y1777
-
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Others
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Infection
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2-Phenylacetophenone has broad-spectrum efflux pump inhibition activity. 2-Phenylacetophenone is a benzoin derivative used as a photoinitiator in vinyl polymerization .
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-
-
- HY-156753
-
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Others
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Cancer
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NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance .
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-
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- HY-N2947
-
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P-glycoprotein
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Infection
Inflammation/Immunology
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Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress .
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-
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- HY-158264
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-
-
- HY-161246
-
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Others
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Neurological Disease
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uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
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-
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- HY-128773
-
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Bacterial
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Infection
|
MRL-494, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
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- HY-128773A
-
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Bacterial
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Infection
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MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
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-
-
- HY-162447
-
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P-glycoprotein
Apoptosis
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Cancer
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P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .
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- HY-144393
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BCRP
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Cancer
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P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel) .
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- HY-143792
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P-glycoprotein
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Neurological Disease
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HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research .
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- HY-139665
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VB124
1 Publications Verification
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Monocarboxylate Transporter
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Cardiovascular Disease
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VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
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-
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- HY-163473
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Bacterial
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Infection
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IITR08367 is a potent effector pump Acinetobacter baumannii Fosfomycin Efflux pump (AbaF) inhibitor for enhancing the antimicrobial activity of Fosfomycin (HY-B1075A) against Acinetobacter baumannii. IITR08367 acts by interfering with Fosfomycin/H + reverse transporter activity. .
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- HY-122416
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Lonchocarpol A; Senegalensin
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BCRP
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Metabolic Disease
Cancer
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6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
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- HY-132301
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MCT4-IN-1
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Monocarboxylate Transporter
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Cancer
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MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research . MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-13766A
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VX-853-2
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Others
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Others
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Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .
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- HY-101444A
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MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride
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Bacterial
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Infection
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PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.
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- HY-B0193A
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Adrenergic Receptor
Autophagy
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Cardiovascular Disease
Endocrinology
Cancer
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Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
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- HY-124819
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Bacterial
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Infection
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D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .
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- HY-157533
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Bacterial
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Others
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AcrB-IN-5 (compound 8) inhibits AcrB and blocks the efflux pump in a dose-dependent manner .
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- HY-100390
-
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BCRP
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Cancer
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(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
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-
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- HY-N10075
-
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P-glycoprotein
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Others
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Euphohelioscopin A is a diterpenoid can be isolated from the Euphorbia helioscopia L. plant. Euphohelioscopin A weakly inhibits P-glycoprotein-mediated efflux of mitoxantrone .
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- HY-119172
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- HY-163454
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Bacterial
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Infection
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NorA-IN-2 (compound DZ-3) is a potent NorA inhibitor. NorA-IN-2 shows NorA efflux pump inhibitors (EPI) activity .
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- HY-157987
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Bacterial
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Infection
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MBX3135 is an efflux pump inhibitor which can enhance the effect of antibiotics through the AcrB target of bacteria. MBX3135 can be used for research of infection and antibiotics .
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- HY-N3308
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Apoptosis
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Cancer
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Medicarpin is a flavonoid isolated from Medicago sativa. Medicarpin induces apoptosis and overcome multidrug resistance in leukemia P388 cells by modulating P-gp-mediated efflux of agents .
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- HY-112220
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Ferroportin
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Metabolic Disease
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VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia .
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- HY-129279
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Farnesyl Transferase
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Cancer
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Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
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- HY-50879
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Elacridar
Maximum Cited Publications
24 Publications Verification
GF120918; GW0918; GG918; GW120918
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P-glycoprotein
BCRP
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Cancer
|
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
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- HY-N2419
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Endogenous Metabolite
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Metabolic Disease
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Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
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- HY-129098
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DMHCA
1 Publications Verification
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LXR
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Metabolic Disease
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DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects and can be used for the research of cholesterol homeostasis diabetes .
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- HY-163079
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FAP
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Cancer
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AlF-PD-FAPI has affinity for FAP , with the IC50 of 0.13 nM, and shows a specific uptake, high internalized fraction, and low cellular efflux in vitro. AlF-PD-FAPI can be used as FAP-targeting tracer .
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- HY-128038
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Opioid Receptor
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Neurological Disease
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N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
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- HY-162144
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Bacterial
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Infection
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BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .
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- HY-157483
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P-glycoprotein
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Cancer
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P-gp inhibitor 18 (compound 6G) is a potent inhibitor of P-gp. P-gp inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .
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-
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- HY-W590664
-
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Endogenous Metabolite
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Cardiovascular Disease
|
C2 Dihydroceramide is a derivative of C2 Ceramide (HY-101180). C2 Dihydroceramide enhances the ABCA1-mediated cholesterol efflux to apolipoprotein A-I (apoA-I) without causing cytotoxicity .
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- HY-50880
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GF120918A
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P-glycoprotein
BCRP
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Cancer
|
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .
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- HY-155048
-
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Bacterial
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Infection
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BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
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- HY-D0067
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DEAC; Coumarin D 1421; D 1421
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Monocarboxylate Transporter
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Cancer
|
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.
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- HY-P3156
-
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Fungal
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Infection
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Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
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-
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- HY-113365
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4-Cholesten-3-one
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Endogenous Metabolite
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Metabolic Disease
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Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells .
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-
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- HY-D2261
-
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Fluorescent Dye
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Metabolic Disease
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BODIPY-cholesterol conjugate-1 (compound 5) is a BODIPY-cholesterol conjugate. BODIPY-cholesterol conjugate-1 is a useful probe for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors . (λex 541 nm, λem 615 nm).
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-
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- HY-N0406
-
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Others
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Inflammation/Immunology
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2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2). Anti-inflammatory effect .
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-
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- HY-126940
-
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Reactive Oxygen Species
P-glycoprotein
Apoptosis
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Cancer
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Furanodiene is a natural terpenoid isolated from Rhizoma Curcumae. Furanodiene plays anti-cancer effects through anti-angiogenesis and inducing ROS production, DNA strand breaks and apoptosis. Furanodiene suppresseed efflux transporter Pgp (P-glycoprotein) function and reduced Pgp protein level .
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-
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- HY-146067
-
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Fungal
Reactive Oxygen Species
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Infection
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β-Nor-lapachone is a Candida glabrata antibiofilm agent. β-Nor-lapachone can stimulate ROS production, inhibits efflux activity, adhesion, biofilm formation and the metabolism of mature biofilms of Candida glabrata. β-Nor-lapachone has antifungal activity .
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-
-
- HY-P2624
-
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PAK
|
Metabolic Disease
|
st-Ht31 is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 induces robust cholesterol/phospholipid efflux. st-Ht31 completely reverses foam cell formation and restores the metabolic health of macrophage .
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- HY-P5878
-
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Biochemical Assay Reagents
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Metabolic Disease
|
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
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- HY-D2262
-
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Fluorescent Dye
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Metabolic Disease
|
BODIPY-cholesterol conjugate-2 (compound 6) is a BODIPY-cholesterol conjugate. BODIPY-cholesterol conjugate-2 is a useful probe for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors. (λex=589 nm, λem=638 nm) .
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- HY-14942
-
RTA 744 free base; WP 744 free base; WP 769
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Others
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Cancer
|
Berubicin (RTA 744 free base; WP 744) is a 4'-O-benzyldoxorubicin that inhibits P-gp and MRP1-mediated efflux and has anticancer activity. Berubicin inhibits glioblastoma multiforme (GBM) and exhibits cytotoxicity. Berubicin has poor bioavailability in mice .
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- HY-17390A
-
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5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
|
Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
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- HY-100928
-
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Calcium Channel
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Neurological Disease
|
YS 035 hydrochloride is a Ca 2+ antagonist on cellular uptake and mitochondrial efflux of calcium ions. YS 035 hydrochloride inhibits Ca 2+ uptake by muscle cells and inhibits Na +/Ca 2+ exchange (Ki=28 µM). YS 035 hydrochloride is a useful tool for research on the mitochondrial Ca 2+ transport .
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- HY-100750
-
-
- HY-135328
-
-
- HY-146117
-
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P-glycoprotein
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Cancer
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P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
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-
- HY-146118
-
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P-glycoprotein
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Cancer
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P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
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-
- HY-16688A
-
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5-HT Receptor
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Neurological Disease
|
RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease .
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- HY-W040150
-
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LXR
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Neurological Disease
Inflammation/Immunology
Cancer
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24S,25-Epoxycholesterol is an agonist for Liver X Receptor (LXR). 24S,25-Epoxycholesterol exhibits properties in regulating the cholesterol efflux , inhibiting tumor growth against gastric cancer and glioblastoma and inducing apoptosis in BMMC cells .
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- HY-B0777
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CL301423
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Antibiotic
BCRP
P-glycoprotein
Parasite
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Infection
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Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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- HY-120574
-
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ADC Cytotoxin
Topoisomerase
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Cancer
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TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
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- HY-144366
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .
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- HY-146389
-
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MDM-2/p53
P-glycoprotein
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Cancer
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Anticancer agent 50 (compound 6) is a potent ABCB1 efflux pump modulator. Anticancer agent 50 shows cytotoxic effects and antiproliferative effects. Anticancer agent 50 decreases the expression of cyclin D1 and induces p53 expression. Anticancer agent 50 has the potential for the research of T-lymphoma .
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- HY-N10512
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Gg4
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Others
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Neurological Disease
|
Gangliotetraose (Gg4) is a tetrasccharide, exhibits major components including GM1 and its sialylated derivatives. GM1 facilitates efflux of nuclear Ca 2+ and reduces the level of nuclear Ca 2+ that characterizes the differentiated neuron. GM1 affects neuronal plasticity and repair mechanisms, as well as neurotrophin release in the brain .
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- HY-157484
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
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- HY-P2624A
-
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PAK
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Metabolic Disease
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st-Ht31 ammonium is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 ammonium induces robust cholesterol/phospholipid efflux. st-Ht31 ammonium completely reverses foam cell formation and restores the metabolic health of macrophage .
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- HY-161645
-
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P-glycoprotein
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Cancer
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P-gp modulator-4 (compound 4c) inhibits the efflux function of P-glycoprotein (P-gp). P-gp modulator-4 shows multidrug resistance (MDR) in cancer reversal activity (IC50 of Paclitaxel (HY-B0015) = 8.80, reversal fold = 211.8) .
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- HY-N4104
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Agaricinic Acid
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Mitochondrial Metabolism
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Metabolic Disease
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Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism .
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- HY-113365S
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4-Cholesten-3-one-d5
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Endogenous Metabolite
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Metabolic Disease
|
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
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- HY-113365S1
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4-Cholesten-3-one-13C
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Endogenous Metabolite
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Metabolic Disease
|
Cholestenone- 13C is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
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- HY-N10069
-
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Others
|
Infection
|
Bonducellin is a a homoisoflavonoid, which can be isolated from Caesalpinia digyna roots. Bonducellin is a potent inhibitor of efflux pump (EP), while EP induces resistance in mycobacteria and serves as a target of anti-TB (tuberculosis) agents. Bonducellin reduces MIC of EtBr by 8-fold against M. smegmatis (MIC=62.5 mg/L) .
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-
- HY-N12320
-
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Antibiotic
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Infection
|
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
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- HY-N0076
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(-)-Bilobalide
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Neurological Disease
|
Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 µM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons .
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- HY-117203A
-
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CDK
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Cancer
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
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- HY-113365S2
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4-Cholesten-3-one-13C2
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Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
|
-
- HY-N12235
-
|
Caspase
|
Inflammation/Immunology
|
Sarglaroids F (compound 6) is an anti-inflammatory agent isolated from the roots of Grass Coral. Sarglaroids F inhibits LPS/ATP-induced IL-1β release by affecting K+ efflux and reducing Caspase-1(P20) levels. Sarglaroids F is not cytotoxic to RAW264.7 cells .
|
-
- HY-135328S
-
-
- HY-101511
-
|
P-glycoprotein
|
Cancer
|
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
|
-
- HY-130244
-
|
Beta-secretase
|
Neurological Disease
|
BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
|
-
- HY-123402
-
GSK3987
1 Publications Verification
|
LXR
|
Metabolic Disease
|
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation .
|
-
- HY-147397
-
|
Pyruvate Kinase
|
Cancer
|
PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
(AC50: the concentration which gives 50% activation of enzyme.)
|
-
- HY-119229
-
|
Others
|
Others
|
VRT-325 is a novel small molecule discovered by screening a compound library designed to address the genetic defect in cystic fibrosis (CF) caused by the ΔF508 mutation in CFTR. VRT-325 belongs to a class of compounds that promote ΔF508-CFTR efflux from the endoplasmic reticulum and restores chloride transport levels in epithelial cells of CF-derived bronchi .
|
-
- HY-147758
-
|
Beta-secretase
Amyloid-β
|
Neurological Disease
|
BACE1/2-IN-1 (compound 34) is a potent BACE1 and BACE2 inhibitor, with an IC50 of 0.01 and 0.0053 μM, respectively. BACE1/2-IN-1 shows a combination of lower Pgp efflux ratio and improved passive permeability. BACE1/2-IN-1 displays reduced liver microsomal metabolic stability .
|
-
- HY-155032
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity,and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015),inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-P3267A
-
|
Ferroportin
Transferrin Receptor
|
Others
|
Apo-Transferrin refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1 .
|
-
- HY-157876
-
|
P-glycoprotein
BCRP
|
Cancer
|
Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
|
-
- HY-17390AR
-
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
|
Loxapine (succinate) (Standard) is the analytical standard of Loxapine (succinate). This product is intended for research and analytical applications. Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .
|
-
- HY-124273
-
L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
|
Endogenous Metabolite
|
Cardiovascular Disease
|
C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
|
-
- HY-U00244A
-
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
|
Cancer
|
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
|
-
- HY-B0777R
-
CL301423 (Standard)
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
|
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-161260
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-151517
-
|
Ras
|
Cancer
|
SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817) .
|
-
- HY-156965
-
|
Others
|
Metabolic Disease
Cancer
|
BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
|
-
- HY-138074
-
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
Milbemycin A4 oxime is a derivative of milbemycin A4 (Item No. 17155) and a component of Milbemycin Oxime (HY-B0778), compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/mL.1 Milbemycin A4 oxime (2.5 μg/mL) blocks efflux of Fluconazole (HY-B0101) from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate Rhodamine 123 (HY-D0816), in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-136071
-
-
- HY-136070
-
-
- HY-128129
-
|
Urea Transporter
|
Metabolic Disease
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
|
-
- HY-149053
-
|
P-glycoprotein
|
Cancer
|
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
|
-
- HY-155198
-
|
Fungal
|
Infection
|
Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (Ki: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
|
-
- HY-136072
-
QPX7728 disodium
|
Bacterial
|
Infection
|
Xeruborbactam (QPX7728) disodium is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam disodium inhibits key serine and metallo beta-lactamases at a nano molar range .
|
-
- HY-P1649B
-
NAB741 acetate
|
Bacterial
Antibiotic
|
Infection
|
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
|
-
- HY-136069
-
QPX7728
|
Bacterial
|
Infection
|
Xeruborbactam (QPX7728) is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam inhibits key serine and metallo beta-lactamases at a nano molar range .
|
-
- HY-P1649
-
NAB741
|
Bacterial
Antibiotic
|
Infection
|
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
|
-
- HY-P1649A
-
NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
|
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
|
-
- HY-N4314
-
4',5,6,7-Tetramethoxyflavone
|
Bacterial
|
Infection
Inflammation/Immunology
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial agent resistance via efflux pump inhibition . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation .
|
-
- HY-B0193AR
-
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
|
-
- HY-149360
-
|
P-glycoprotein
|
Cancer
|
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells .
|
-
- HY-108694
-
|
Endogenous Metabolite
NF-κB
|
Metabolic Disease
Inflammation/Immunology
|
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
|
-
- HY-139426
-
ML-SI3 (cis/trans mix)
|
Parasite
TRP Channel
|
Cardiovascular Disease
Neurological Disease
|
ML-SI3 is a mixture of cis/trans ML-SI3 (HY-139426A), which is a TRPML1/2 channel inhibitor with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy. The cis/trans ML-SI3 (HY-139426A) components of ML-SI3 are TRPML2 activators with EC50s of 3.3 μM and 9.4 μM, respectively .
|
-
- HY-N0686
-
-
- HY-124187
-
Ethyl pinolenate
|
Biochemical Assay Reagents
|
Others
|
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
|
-
- HY-101453
-
|
Others
|
Cancer
|
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .
|
-
- HY-W013712
-
|
Potassium Channel
|
Neurological Disease
|
GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect .
|
-
- HY-W127487
-
|
Biochemical Assay Reagents
|
Others
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.
|
-
-
-
HY-L049
-
|
1,345 compounds
|
Antibacterial agents are a group of materials that fight against pathogenic bacteria. Thus, by killing or reducing the metabolic activity of bacteria, their pathogenic effect in the biological environments will be minimized. The most widely used antibacterial agents exert their effects on bacterial cell wall synthesis, protein synthesis, DNA replication and metabolic pathways. However, resistance to antimicrobial agents has become a major source of morbidity and mortality worldwide. The main mechanisms of resistance are limiting uptake of a drug, modification of a drug target, inactivation of a drug, and active efflux of a drug. Therefore, it is an urgent need to develop new drugs targeted at resistant organisms.
MCE offers a unique collection of 1,345 compounds with validated antibacterial activities. MCE antibacterial compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L048
-
|
352 compounds
|
The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins, overexpression and changes in drug targets and biofilm formation, emphasizing the importance of discovering new antifungal drugs and therapies. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, such as the combination of antifungal drugs, development of new formulations for antifungal agents and modifications to the chemical structures of traditional antifungals, etc.
MCE offers a unique collection of 352 compounds with validated antifungal activities. MCE antifungal compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
|
-
-
HY-L169
-
|
394 compounds
|
Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 394 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
|
Cat. No. |
Product Name |
Type |
-
- HY-D2262
-
|
Dyes
|
BODIPY-cholesterol conjugate-2 (compound 6) is a BODIPY-cholesterol conjugate. BODIPY-cholesterol conjugate-2 is a useful probe for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors. (λex=589 nm, λem=638 nm) .
|
-
- HY-D2341
-
|
Fluorescent Dyes/Probes
|
6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors .
|
Cat. No. |
Product Name |
Type |
-
- HY-P3267A
-
|
Native Proteins
|
Apo-Transferrin refers to iron free Transferrin (HY-P3267), serves as Transferrin receptor ligand and mediates iron release from endothelial cells. Apo-Transferrin indicates an iron deficient environment, can directly bind to hephaestin, which can convert Fe 2+ to Fe 3+. Apo-Transferrin mediates iron efflux most likely in cooperation with ferroportin 1 .
|
-
- HY-124187
-
Ethyl pinolenate
|
Biochemical Assay Reagents
|
Pinolenic acid is a polyunsaturated fatty acid found in the seed oils of red pine (Pinus orientalis) and maritime pine (Pinus pinaster). Both oils were found to have lipid-lowering properties. A diet containing marine pine nut oil (MPSO) reduces HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to reduce cholesterol efflux in vitro. Korean pine nut oil supplements may help obesity by reducing appetite. People who take this oil experience an increase in the satiety hormones CCK and GLP-1 and a decrease in appetite. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not metabolized to arachidonic acid and can reduce the level of arachidonic acid in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.
|
-
- HY-W127487
-
|
Biochemical Assay Reagents
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C18-HSL, one of four lipophilic long acyl side chain AHLs produced by the LuxI AHL synthase homolog SinI, is involved in quorum-sensing signaling in strains of Rhizobium meliloti (a nitrogen-fixing bacterial symbiont of the legume M. sativa) . C18-HSL and other hydrophobic AHLs tend to localize in the relatively lipophilic environment of bacterial cells and cannot diffuse freely across the cell membrane. Long-chain N-acyl homoserine lactones can be exported from cells by efflux pumps, or can be transported between communicating cells by extracellular outer membrane vesicles.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2576
-
|
Bacterial
|
Infection
|
Polistes mastoparan is an antimicrobial peptide. Polistes mastoparan increases S. aureus cell K + efflux and inhibits cell viability with EC50 of 5 μM .
|
-
- HY-P5901
-
-
- HY-P3156
-
|
Fungal
|
Infection
|
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
|
-
- HY-P2624
-
|
PAK
|
Metabolic Disease
|
st-Ht31 is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 induces robust cholesterol/phospholipid efflux. st-Ht31 completely reverses foam cell formation and restores the metabolic health of macrophage .
|
-
- HY-P5878
-
|
Biochemical Assay Reagents
|
Metabolic Disease
|
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
|
-
- HY-P2624A
-
|
PAK
|
Metabolic Disease
|
st-Ht31 ammonium is a membrane-permeable peptide inhibitor of protein kinase A (PKA) anchoring. st-Ht31 ammonium induces robust cholesterol/phospholipid efflux. st-Ht31 ammonium completely reverses foam cell formation and restores the metabolic health of macrophage .
|
-
- HY-P1649B
-
NAB741 acetate
|
Bacterial
Antibiotic
|
Infection
|
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
|
-
- HY-P1649
-
NAB741
|
Bacterial
Antibiotic
|
Infection
|
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
|
-
- HY-P1649A
-
NAB741 TFA
|
Bacterial
Antibiotic
|
Infection
|
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N2947
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-
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- HY-N3308
-
-
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- HY-122416
-
-
-
- HY-N10075
-
-
-
- HY-129279
-
-
-
- HY-N2419
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-
-
- HY-113365
-
-
-
- HY-N0406
-
-
-
- HY-126940
-
-
-
- HY-N10512
-
-
-
- HY-N4104
-
-
-
- HY-N10069
-
-
-
- HY-N12320
-
-
-
- HY-N0076
-
-
-
- HY-N12235
-
-
-
- HY-N4314
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4',5,6,7-Tetramethoxyflavone
|
Infection
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Plants
Compositae
Inflammation/Immunology
Disease Research Fields
Genista maderensis (Webb & Berthel.) Lowe
|
Bacterial
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive component of Siam weed extract. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) exhibits anti-inflammatory activity through NF-κB pathway . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) modulats of bacterial agent resistance via efflux pump inhibition . Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) can enhance blood coagulation .
|
-
-
- HY-108694
-
-
-
- HY-N0686
-
-
Cat. No. |
Product Name |
Chemical Structure |
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- HY-113365S
-
|
Cholestenone-d5 is the deuterium labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
|
-
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- HY-113365S1
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|
Cholestenone- 13C is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
|
-
-
- HY-113365S2
-
|
Cholestenone- 13C2 is the 13C labeled Cholestenone. Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells[1][2][3].
|
-
-
- HY-135328S
-
|
Norverapamil-d7 is a deuterium labeled Norverapamil ((±)-Norverapamil). Norverapamil, an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].
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