AMPK-IN-3 (化合物 67) 是一种强效的、选择性的 AMPK 抑制剂,其对AMPK (α2)、AMPK (α1) 和 KDR 的 IC50 值分别为 60.7、107 和 3820 nM。AMPK-IN-3 对 AMPK 的抑制不影响细胞活力或导致 K562 细胞的明显细胞毒性。AMPK-IN-3 可用于癌症的研究。
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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].
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.
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