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 IC 50 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.

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IC50: 1.4 nM (AMPK kinase,10 μM ATP), 15 nM (AMPK kinase, 2 mM ATP), 1324 nM (Aurora A), 124 nM (Flt3), 788 nM (c-Met), 36 nM (Rsk4)

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) signif

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4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Lemos C, et al. The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cell Oncol (Dordr). 2021 Jun;44(3):581-594.

In Vitro: DMSO : 25 mg/mL (53.36 mM; ultrasonic and warming and heat to 60°C)配制储备液