1684386-71-7
1684386-71-7 结构式
基本信息
N-[4-(2-氯-5-甲基-4-嘧啶基)苯基]-N-[[4-[[(2,2-二氟乙酰基)氨基]甲基]苯基]甲基]-2,4 -二羟基-苯甲酰胺
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
Benzamide, N-[4-(2-chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxy-
物理化学性质
DMSO:2.0(Max Conc. mg/mL);3.62(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.9(Max Conc. mM)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-12492 | 1684386-71-7 VER-246608 | 1684386-71-7 | 1mg | 636元 |
| 2024/04/30 | HY-12492 | 1684386-71-7 VER-246608 | 1684386-71-7 | 5mg | 1400元 |
| 2024/04/30 | HY-12492 | 1684386-71-7 VER-246608 | 1684386-71-7 | 10mM * 1mLin DMSO | 1710元 |
常见问题列表
IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)
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 Ser 293 residue of E1α (phosphorylated by all four PDK isozymes) with IC 50 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.