1684386-71-7

1684386-71-7化学性质

沸点 :830.4±65.0 °C(Predicted)
密度 :1.414±0.06 g/cm3(Predicted)
溶解度 :DMF:2.0(Max Conc. mg/mL);3.62(Max Conc. mM)
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)
形态 :A solid
酸度系数(pKa) :7.61±0.35(Predicted)
颜色 :White to off-white

1684386-71-7性质、用途与生产工艺

生物活性 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 35 nM，40 nM，84 nM 和 91 nM。
靶点

IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)
体外研究

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.

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