产品
编 号:F751734
分子式:C27H25FN6O
分子量:468.53
产品类型
结构图
CAS No: 2377576-35-5
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产品详情
生物活性:
BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 μM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.
体外研究:
BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50 values of 1.4 nM at low, 10 μM ATP concentration and 15 nM at high, 2 mM ATP concentration.BAY-3827 (0-200 μM) inhibits Aurora A, Flt3, c-Met and Rsk4 with IC50 values of 1324, 124,788 and 36 nM , respectively with 10 μM ATP concentration.BAY-3827 (overnight) strongly reduces ACC1 Ser79 phosphorylation in LNCaP and VCaP cells, and shows a lesser extent in IMR-32 and especially in Colo320 cells.BAY-3827 (0-10 nM; 6 d) shows strong inhibitory effects to LNCaP and VCaP cells.BAY-3827 (1 and 5 μM; 24 and 48 h) represses LIPE gene expression, reduces serine/threonine kinase AKT3 and blocks the expression of several genes from the mitochondrial carnitine palmitoyltransferase (CPT) family which is involved in acyl carnitine formation in VCaP cells.BAY-3827 (5 μM; 2-4 d) significantly increases the formation of lipid droplets in comparison to androgen treatment only.