AMPK-IN-3

AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer[1].

Signaling Pathways >> Epigenetics >> AMPK

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> AMPK

AMPK (α2):60.7 nM (IC50)

AMPK (α1):107 nM (IC50)

KDR:3820 nM (IC50)

AMPK-IN-3 (100 nM) shows inhibition values for AMPK(α2), FLT1, JAK1 JH2-pseudokinase and AMPK(α1) for 64%, 43%, 41% and 29%, respectively[1]. AMPK-IN-3 (0.195313, 0.78125, 3.125, 12.5, 50 µM; 2 h) decreases the level of p-ACC in K562 cells[1]. AMPK-IN-3 (1-100 µM; 24, 48, 72 h) shows potent inhibition of cellular AMPK activity but not affect cell viability[1]. Cell Viability Assay[1] Cell Line: K562 cells Concentration: 0.195313, 0.78125, 3.125, 12.5, 50 µM Incubation Time: 2 h Result: Decreased cellular levels of p-ACC(Ser79) in K562 cells. Cell Viability Assay[1] Cell Line: K562 cells Concentration: 1-100 µM Incubation Time: 24, 48, 72 h Result: Showed no measurable impact on cell viability in K562 cells cultured under hypoxic conditions for 72 hours.

[1]. Matheson CJ, et al. Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. Eur J Med Chem. 2020 Jul 1;197:112316.