BAY-3827 B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAY-3827 是强效的、选择性的 AMPK 抑制剂，IC50 值为 1.4 nM (10 μM ATP) 和 15 nM (2 mM ATP)。BAY-3827 对其他 331 种被测激酶的选择性超过 500 倍相比于 AMPK。AMPK 抑制乙酰 CoA 羧化酶 1 的磷酸化，并在雄激素依赖的前列腺癌细胞株中显示出强效的抗增殖活性。

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.

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.Cell Proliferation Assay Cell Line:LNCaP, VCaP, 22Rv1, C4-2B, PC-3 and DU-145 prostate cancer cell lines Concentration:0-10 nM Incubation Time:6 d Result:Showed strong inhibitory effects for LNCaP and VCaP cells, two prostate cancer cell lines with IC50 values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC50 value of 5.55 nM.

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Others

Other Targets

Acyltransferase | AMPK

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2377576-35-5

468.53

C27H25FN6O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (53.36 mM; 超声助溶 (<60°C)

C(#N)C=1C(C(C#N)=C(C)N(C)C1C)C=2C=C3C(=C(C)C2F)NN=C3NC(=O)C4=C(CC)C=CC=C4

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(-20℃)

With Ice Pack

≥ 2 years