Signaling Pathway

AMPK

AMPK

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AMPK (AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. It consists of three proteins (subunits) that together make a functional enzyme. The net effect of AMPK activation is stimulation of hepatic fatty acid oxidation andketogenesis, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, stimulation of skeletal muscle fatty acid oxidation and muscle glucose uptake, and modulation of insulin secretion by pancreatic beta-cells. AMPK acts as a metabolic master switch regulating several intracellular systems including the cellular uptake of glucose, the β-oxidation of fatty acids and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria.

AMPK Inhibitors & Modulators (17)

Product Name Catalog No. Brief Description
A-769662

HY-50662

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.

AICAR

HY-13417

AICAR (Acadesine), is an AMP-activated protein kinase activator, which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes.

AICAR phosphate

HY-13417A

AICAR phosphate (Acadesine), is an AMP-activated protein kinase activator, which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes.

Ampkinone

HY-12831

Ampkinone is a small molecule activator of AMPK; stimulate functional activation of AMPK via the phosphorylation at Thr172 in cultured L6 muscle cells with an EC50 value of 4.3 μM, enhancing glucose uptake by 3.2-fold.

Dorsomorphin

HY-13418A

Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK 6).

Dorsomorphin dihydrochloride

HY-13418

Dorsomorphin 2Hcl (Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK 6).

ETC-1002

HY-12357

ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

HTH-01-015

HY-12334

HTH-01-015 is a potent and selective inhibitor of NUAK1 with IC50 of 100 nM, does not significantly inhibit NUAK2 (IC50 of >10 μM).

Imeglimin

HY-14771

Imeglimin(EMD-387008) is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins; It has been shown to act on the liver, muscle and pancreatic β-cells to uniquely target the key defects of type 2 diabetes.

Imeglimin hydrochloride

HY-14771A

Imeglimin(EMD 387008) is the first in a new tetrahydrotriazine-containing class of oral antidiabetic agents, the glimins.

Latrepirdine dihydrochloride

HY-14537

Latrepirdine (dihydrochloride) is a potent activator of AMPK, also an anti-histamine, promote the removal of α-synuclein protein aggregates.

Metformin hydrochloride

HY-17471A

Metformin Hcl, a widely used anti-diabetic drug has potential efficacy as an anti-cancer drug.

Phenformin hydrochloride

HY-16397A

Phenformin, an anti-diabetic drug, has demonstrated antitumor activity both in vitro and in vivo.

WZ4003

HY-15802

WZ4003 is a first potent and highly specific protein kinase inhibitor of NUAK kinases with IC50 of 20 nM/100 nM for NUAK1/NUAK2; no significant inhibition on 139 other kinases.

YLF-466D

HY-15840

YLF-466D is an allosteric AMPK activator.

ZLN024

HY-16708

ZLN024 is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM.

ZLN024 hydrochloride

HY-16708A

ZLN024 Hcl is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM.