AP-1

Activator Protein 1

Activator Protein 1 (AP-1) is not a single protein, but a collective term referring to dimeric transcription factors composed of Jun (c-Jun, JunB, JunD), Fos (c-Fos, FosB, Fra-1, Fra-2) ATF (activating transcription factor, ATF-2, ATF-3/LRF1, ATF-4, ATF-5, ATF-6B, ATF-7, BATF, BATF-2, BATF-3, JDP2) or MAF (c-MAF, MafA, MafB, MafF, MafG, MafK and Nrl) subunits that bind to a common DNA site, the AP-1-binding site. AP-1 is involved in a plethora of cellular and physiological functions. It is acknowledged as a master integrator of a myriad of extracellular signals allowing cells to adapt to changes in their environment. AP-1 has also been implicated in various severe diseases. These include transplant rejection, fibrosis, organ injury and a variety of inflammatory pathologies such as rheumatoid arthritis, asthma and psoriasis. In addition, cancer is undoubtedly the most documented pathology involving AP-1 where its activity is often dysregulated and contributes to cell transformation, tumor progression, aggressiveness and resistance to treatments.

AP-1 Inhibitors (13)

AP-1 Related Products (19):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-12270

T-5224	Inhibitor	99.59%
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

HY-15870

SR 11302		98.91%
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).

HY-19357

E3330	Inhibitor	99.34%
E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.

HY-N0716B

Berberine sulfate	Inhibitor	≥98.0%
Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability.

HY-121607

INI-43		99.92%
INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G₂-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway.

HY-N0719

Fargesin		99.91%
Fargesin is a bioactive neolignan isolated from magnolia plants, with antihypertensive and anti-inflammatory effects.

HY-141645

IMM-H007	Inhibitor
IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.

HY-N4226

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid		99.96%
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function.

HY-N1513

Ganoderic acid H	Inhibitor	99.68%
Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling.

HY-P99323

Timolumab	Inhibitor	98.56%
Timolumab (BTT1023 ), a recombinant fully human monoclonal antibody that specifically binds VAP-1. Timolumab (BTT1023 ) could be used in the study of chronic inflammatory diseases.

HY-N10913

Chloranthalactone B	Inhibitor
Chloranthalactone B, a lindenane-type sesquiterpenoid, is a nature product that could be isolated from Chinese medicinal herb Sarcandra glabra. Chloranthalactone B inhibits the production of inflammatory mediators by inhibiting the AP-1 and p38 MAPK pathways.

HY-151876

Glucocorticoid receptor modulator 1	Inhibitor	99.79%
Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC₅₀ value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.

HY-N10926

(+)-Glaucarubinone	Inhibitor
(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC₅₀ value of 0.13 µM. (+)-Glaucarubinone shows noncytotoxic.

HY-P99526

Vapaliximab	Inhibitor
Vapaliximab (2D10) is a monoclonal antibody against human VAP-1.

HY-103323

Fas C-Terminal Tripeptide
Fas C-Terminal Tripeptide is a C-terminal tripeptide of Fas. Fas C-Terminal Tripeptide shows the inhibitory effect on Fas/FAP-1 binding.

HY-10072

SPC 839	Inhibitor
SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC₅₀ of 0.008 μM.

HY-142444

SSAO/VAP-1 inhibitor 1
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).

HY-N0716

Berberine	Inhibitor
Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.

HY-N3261

Methyllinderone	Inhibitor
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis.

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