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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Pyruvate Dehydrogenase Kinase (PDK)-VER-246608
VER-246608

Chemical Structure : VER-246608

CAS No.: 1684386-71-7

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VER-246608 (VER246608)

货号: PC-24275Not For Human Use, Lab Use Only.

VER-246608 is a potent, pan-isoform ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK, PDHK) with IC50 of 35 nM, 40 nM, 84 nM, and 91 nM for PDHK1, PDHK3, PDHK2, and PDHK4, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

VER-246608 is a potent, pan-isoform ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK, PDHK) with IC50 of 35 nM, 40 nM, 84 nM, and 91 nM for PDHK1, PDHK3, PDHK2, and PDHK4, respectively.
VER-246608 increases pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity.
VER-246608 is weakly anti-proliferative to cancer cells in standard culture media; however, depletion of either serum or combined D-glucose/L-glutamine resulted in enhanced cellular potency.
VER-246608 potentiates the activity of doxorubicin.
VER-246608 disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.

物理化学性质&存储条件

分子量 552.96
分子式 C28H23ClF2N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-(2-Chloro-5-methylpyrimidin-4-yl)phenyl)-N-(4-((2,2-difluoroacetamido)methyl)benzyl)-2,4-dihydroxybenzamide

参考文献

1. Moore JD, et al. Oncotarget. 2014 Dec 30;5(24):12862-76.

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