BAY-3827 B

Research use only, not for human use.

BAY-3827 is a potent and selective AMPK inhibitor with potential antitumor activity, demonstrating antiproliferative effects in an androgen-dependent prostate cancer model and inhibiting the phosphorylation of acetyl CoA carboxylase 1 (ACC-1).

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 : 25 mg/mL (53.36 mM; Ultrasonic (<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