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VER-246608
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VER-246608图片
CAS NO:1684386-71-7
规格:98%
分子量:552.96
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
VER-246608是一种有效的,ATP竞争性的丙酮酸脱氢酶激酶(PDK)抑制剂,抑制PDK-1,PDK-3,PDK-2,和PDK-4,IC50分别为35nM,40nM,84nM和91nM。
CAS:1684386-71-7
分子式:C28H23ClF2N4O4
分子量:552.96
纯度:98%
存储:Store at -20°C

Background:

VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.


VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser293 residue of E1α (phosphorylated by all four PDK isozymes) with IC50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth[1].



[1]. Moore JD, et al. VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget. 2014 Dec 30;5(24):12862-76.