| Cat. No. |
Product Name |
CAS No. |
Information |
| GY06967 |
AMPK-Activator-13
|
1243184-62-4 |
A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM); inhibits de novo lipogenesis in cellular and animal models of hyperlipidemia; the cell-permeable prodrug of compound 2 (AMPK-Activator-2). |
| GY06962 |
EX-229
|
1219739-36-2 |
EX-229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM; induces AMPK activation and glucose uptak in a wortmannin-independent manner; increases fatty acid oxidation in L6 myotubes. |
| GY06954 |
PF-739
|
1852452-14-2 |
PF-739 is a novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 121 nM, potently inhibits de novo lipogenesis (IC50=25 nM) in primary rat hepatocytes; increases PGC1a transcription and mitochondrial content, effectively activats AMPK in hepatocytes and in skeletal muscle; caused a rapid lowering of plasma glucose levels with no impact on hepatic glucose production in diabetic mice. |
| GY06953 |
MK-8722
|
1394371-71-1 |
MK-8722 is a potent, selective, allosteric pan-AMPK activator with EC50 of 1-60 nM for all 12 mammalian AMPK isoforms; exhibits higher affinity for β1-containing (1-6 nM) versus β2-containing (15-63 nM) pAMPK complexes; increases glucose uptake into skeletal muscle in vitro and in vivo, but induces cardiac hypertrophy. |
| GY06868 |
PF-06885249
|
1467059-70-6 |
PF-06685249 is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 12 nM for α1β1γ1-AMPK, shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3); demonstrates in vivo target engagement experiment in ZSF-1 rats, an obese/diabetic rodent model of diabetic nephropathy. |
| GY10045 |
BL-AD008
|
|
BL-AD008 (BL-AD 008) is a novel small molecule, dual-target activator targeting AMPK/ZIPK; demonstrates remarkable anti-proliferative activities toward cervical cancer cells and could induce apoptosis by death-receptor and mitochondrial pathways; also shows anti-tumor activities and induces apoptosis by targeting AMPK/ZIPK in vivo. |
| GY03481 |
AICAR phosphate
|
681006-28-0 |
AICAR phosphate (Acadesine, AICA Riboside, NSC 105823) is a selective AMPK activator in both hepatocytes and adipocytes; inhibits the synthesis of fatty acids and sterols and inactivates HMG-CoA reductase in rat hepatocytes at 0.5 mM, inhibits insulin-stimulated glucose and reduces GLUT4 translocation in 3T3-L1 adipocytes; down-regulates the insulin receptor expression in HepG2 cells. |
| GY04309 |
A-769662
|
844499-71-4 |
A-769662 is a small molecule AMPK activator that directly stimulates partially purified rat liver AMPK (EC50=0.8 uM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50=3.2 uM); decreases hepatic expression of PEPCK, G6Pase, and FAS, lowered plasma glucose by 40%, reduces body weight gain and significantly decreases both plasma and liver triglyceride levels in ob/ob mice (30 mg/kg b.i.d.); also directly inhibits Na(+)-K(+)-ATPase, decreases the sodium pump cell surface abundance in L6 skeletal muscle cells. |
| GY01720 |
HTH-01-015
|
1613724-42-7 |
HTH-01-015 is a potent, specific NUAK1 (AMPK-related kinase 5, ARK5) inhibitor with IC50 of 100 nM, displays >100-fold higher potency than NUAK2; also does not markedly suppress the activity of any of the other 139 protein kinases, including AMPK; suppresses NUAK1-mediated MYPT1 phosphorylation in vivo, the NUAK1 mutation (A195T) renders resistant to HTH-01-015; significantly inhibits migration the proliferation of MEFs (mouse embryonic fibroblasts). |
| GY01246 |
Dorsomorphin
|
866405-64-3 |
Dorsomorphin (BML-275, Compound C) is a potent, selective and reversible AMPK inhibitor with Ki of 109 nM, shows no no significant activity on ZAPK, SYK, PKCθ, PKA and JAK3; inhibits AMPK activation induced by AICAR and Metformin, also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6); promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro, induces autophagy in cancer cell lines via a mechanism independent of AMPK inhibition. |
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