BMS-3

生物活性靶点体外研究 BMS-3 试剂级价格

CAS号:1338247-30-5
英文名:N-(5-(1-(2,6-dichlorophenyl)-3-(difluoroMethyl)-1H-pyrazol-5-yl)thiazol-2-yl)cyclopropanecarboxaMide
中文名:BMS-3
CBNumber:CB42598622
分子式:C17H12Cl2F2N4OS
分子量:429.27
MOL File:1338247-30-5.mol

BMS-3化学性质

密度 :1.69±0.1 g/cm3(Predicted)
储存条件 :Sealed in dry,Store in freezer, under -20°C
溶解度 :DMF: 15 mg/ml; DMSO: 25mg/ml; DMSO:PBS (pH 7.2)(1:5): 0.2 mg/ml; Ethanol: 1 mg/ml
形态 :A crystalline solid
酸度系数(pKa) :8.28±0.70(Predicted)
颜色 :White to off-white

BMS-3性质、用途与生产工艺

生物活性 BMS-3 是一种高效的 LIMK 抑制剂，抑制 LIMK1 和 LIMK2，IC50 分别为 5 nM 和 6 nM。
靶点

LIMK1

5 nM (IC ₅₀ )

LIMK2

6 nM (IC ₅₀ )
体外研究

BMS-3 (Compound 2) causes a dose-dependent reduction in cell count and induces mitotic arrest by increases in total nuclear DNA intensity and histone H3 phosphorylation after 24 h treatment in A549 human lung cancer cells. BMS-3 inhibits A549 human lung cancer cells with EC ₅₀ value of 154 nM. BMS-3 is used to demonstrate the direct participation of LIMK1 in the phosphorylation of Cofilin. Inhibition of p-LIMK with 1-50 μM of BMS-3 results in a dose-dependent decrease of p-Cofilin after 10 min incubation in capacitating conditions. As a control, sperm are also incubated for 10 min under non-capacitating conditions which result in low levels of p-Cofilin. In the presence of 1 or 50 μM of BMS-3, actin polymerization levels are significantly lower compared to controls (DMSO). Mouse sperm are incubated under capacitating conditions for 90 min in the presence or absence of increasing concentrations of p-LIMK inhibitor BMS-3 (0, 1, 10 and 50 μM). The increasing concentrations of BMS-3 result in a strong decrease on the percentage of sperm that undergoes acrosomal exocytosis after stimulation with 20 μM of Progesterone.