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。
| 生物活性 | BAY-3827 is a potent and selectiveAMPKinhibitor withIC50values 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 ofacetyl-CoA carboxylase1 and shows strongest anti-proliferative activity in androgen-dependent prostatecancercell lines[1]. |
| IC50& Target | 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)[1] |
体外研究
(In Vitro) | BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50values of 1.4 nM at low, 10 μM ATP concentration and 15 nM at high, 2 mM ATP concentration[1].
BAY-3827 (0-200 μM) inhibits Aurora A, Flt3, c-Met and Rsk4 with IC50values of 1324, 124, 788 and 36 nM , respectively with 10 μM ATP concentration[1].
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[1].
BAY-3827 (0-10 nM; 6 d) shows strong inhibitory effects to LNCaP and VCaP cells[1].
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[1].
BAY-3827 (5 μM; 2-4 d) significantly increases the formation of lipid droplets in comparison to androgen treatment only[1].
Cell Proliferation Assay[1] | 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 IC50values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC50value of 5.55 nM. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(53.36 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.1343 mL | 10.6717 mL | 21.3434 mL | | 5 mM | 0.4269 mL | 2.1343 mL | 4.2687 mL | | 10 mM | 0.2134 mL | 1.0672 mL | 2.1343 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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