AMPK/Akt

Pathways Recommended:	PI3K/Akt/mTOR

By Targets:	Akt (6) AMPK (7) Apoptosis (5) Aurora Kinase (2) Autophagy (5) Bcl-2 Family (1) Beta-secretase (2) Caspase (1) Cholinesterase (ChE) (2) EGFR (1) Endogenous Metabolite (1) ERK (1) HDAC (1) JNK (1) Keap1-Nrf2 (1) mTOR (2) NF-κB (1) NO Synthase (1) Parasite (1) PARP (1) PKA (1) PKC (1) Reactive Oxygen Species (2) Sirtuin (1)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Inflammation/Immunology (3) Metabolic Disease (7) Neurological Disease (3)

Targets Recommended: AMPK Akt

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N7676

Marein	AMPK HDAC	Cardiovascular Disease Neurological Disease Metabolic Disease
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC₅₀ of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects .

HY-10249

GSK-690693 25+ Cited Publications	Akt AMPK Autophagy	Cancer
GSK-690693 is an ATP-competitive *pan-Akt* inhibitor with IC₅₀s of 2 nM, 13 nM, 9 nM for *Akt1, Akt2* and *Akt3, respectively. GSK-690693 is also an AMPK* inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation .

HY-W013816

Dipentyl phthalate	AMPK Akt	Metabolic Disease
Dipentyl phthalate is an endocrine-disrupting phthalate plasticizer. Dipentyl phthalate increases AMPK phosphorylation and decreases AKT1 phosphorylation and SIRT1 levels. Dipentyl phthalate reduces adrenocorticotropic hormone levels. Dipentyl phthalate is a testicular toxicant .

HY-126307

Urolithin B 3 Publications Verification	NF-κB JNK ERK Akt AMPK Endogenous Metabolite	Inflammation/Immunology
Urolithin B is one of Ellagitannins' slow microbial products, and has anti-inflammatory and anti-inflammatory effects. Urolithin B suppresses NF-κB activity. Urolithin B suppresses JNK, ERK and *Akt's oxidation, and increases AMPK*'s oxidation. Urolithin B is also a quantitative change factor for bone and skin quality.

HY-N3426

Kazinol B	NO Synthase Akt AMPK	Metabolic Disease
Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research .

HY-10971A

Alisertib sodium MLN 8237 sodium	Aurora Kinase Autophagy Apoptosis	Cancer
Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the *AKT/mTOR/AMPK/p38* pathway in leukemic cells. Antitumor activity .

HY-10971

Alisertib Maximum Cited Publications 39 Publications Verification MLN 8237	Aurora Kinase Autophagy Apoptosis	Cancer
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the *AKT/mTOR/AMPK/p38* pathway in leukemic cells. Antitumor activity .

HY-N12386

SIRT1 activator 1	Sirtuin	Cancer
SIRT1 activator 1(compound 3) is a derivative of marine compound xyloallenoide A isolated from the mangrove fungus Xylaria sp.SIRT1 activator 1 shows angiogenic activities in zebrafish. SIRT1 activator 1 protects hEPC against AngII-induced senescence by increasing SIRT1 expression levels and balancing the AMPK/Akt signaling pathway .

HY-N2447

Amarogentin 2 Publications Verification	AMPK Apoptosis	Metabolic Disease Cancer
Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating *AMPK* .

HY-W009731

Dibenzoylmethane	Keap1-Nrf2	Metabolic Disease Cancer
Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 .

HY-P10298

RA-XII	Autophagy Apoptosis Akt mTOR	Inflammation/Immunology Cancer
RA-XII is bicyclic hexapeptidic glucoside , which exhibits antitumor and anti-inflammatory activity. RA-XII activates Akt-mTOR singaling pathway, inhibits the formation of autophagosomes, and thus suppresses autophagy. RA-XII induces apoptosis through AMPK/mTOR/P70S6K pathway. RA-XII inhibit metastasis via reducing cell adhesion and invasion in breast cancer cells. RA-XII attenuates anti-inflammatory efficacy against acute kidney injury through HO-1/Nrf2 pathway .

HY-N0226

Epiberberine	Cholinesterase (ChE) Beta-secretase	Neurological Disease Metabolic Disease
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .

HY-N0226A

Epiberberine chloride 4 Publications Verification	Cholinesterase (ChE) Beta-secretase Reactive Oxygen Species	Neurological Disease Metabolic Disease
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC₅₀s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO ^- scavenging effect (IC₅₀, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .

HY-N0281

Daphnetin 3 Publications Verification 7,8-Dihydroxycoumarin	EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite	Inflammation/Immunology Cancer
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .

Cat. No.	Product Name

HY-L015

PI3K/Akt/mTOR Compound Library	587 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 587 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

PI3K/Akt/mTOR Compound Library

587 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 587 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Cat. No.	Product Name	Target	Research Area