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BMS-3

BMS-3

产品编号 T4600   CAS 1338247-30-5

BMS3 是一种有效的 LIMK 抑制剂,抑制 LIMK1和 LIMK2的 IC50分别为 5 nM 和 6 nM。

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BMS-3 Chemical Structure
BMS-3, CAS 1338247-30-5
规格 价格/CNY 货期 数量
1 mg ¥ 298 现货
2 mg ¥ 423 现货
5 mg ¥ 747 现货
10 mg ¥ 1,160 现货
25 mg ¥ 2,080 现货
50 mg ¥ 3,490 现货
100 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 763 现货
其他形式的 BMS-3:
产品目录号及名称: BMS-3 (T4600)
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纯度: 99.31%
纯度: 99.19%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 BMS-3 is a potent LIMK inhibitor with IC50s of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.
靶点活性 LIMK1:5 nM, LIMK2:6 nM
体外活性 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 EC50 value of 154 nM[1]. 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 pLIMK 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[2] .
激酶实验 The protein kinase domains of human LIMK1 and LIMK2 are expressed as glutathione S-transferase fusion proteins using the Bac-to-Bac system in Sf9 cells. Compounds 1 to 6 (e.g., BMS-3) are assayed for inhibition of LIMK1 and LIMK2 protein kinase activity by radioactive phosphate incorporation into biotinylated full-length human destrin. Reactions are done with a concentration series of compound in 25 mM HEPES, 100 mM NaCl, 5 mM MgCl2, 5 mM MnCl2, 1 μM total ATP, 83 μg/mL biotinylated destrin, 167 ng/mL glutathione S-transferase-LIMK1, or 835 ng/mL glutathione S-transferase-LIMK2 in a total volume of 60 μL at room temperature for 30 min (LIMK1) or 60 min (LIMK2). Reactions are terminated by addition of 140 μL of 20% TCA/100 mM sodium pyrophosphate, and the precipitates are harvested onto GF/C unifilter plates. The radioactivity incorporated is determined using a TopCount after addition of 35 μL Microscint scintillation fluid[1]
分子量 429.27
分子式 C17H12Cl2F2N4OS
CAS No. 1338247-30-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 27.5 mg/mL (64.06 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3295 mL 11.6477 mL 23.2954 mL 58.2384 mL
5 mM 0.4659 mL 2.3295 mL 4.6591 mL 11.6477 mL
10 mM 0.233 mL 1.1648 mL 2.3295 mL 5.8238 mL
20 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9119 mL
50 mM 0.0466 mL 0.233 mL 0.4659 mL 1.1648 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Ross-Macdonald P, et al. Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors. Mol Cancer Ther. 2008 Nov;7(11):3490-8. 2. Romarowski A, et al. PKA-dependent phosphorylation of LIMK1 and Cofilin is essential for mouse sperm acrosomal exocytosis. Dev Biol. 2015 Sep 15;405(2):237-49.
LY2812223 LX7101 BMS-5 SM1-71 T56-LIMKi R-10015 TH-257 LIMK-IN-22j

相关化合物库

该产品包含在如下化合物库中:
经典已知活性库 抑制剂库 已知活性化合物库 激酶抑制剂库 抗癌化合物库 NO PAINS 化合物库 抗衰老化合物库 表型筛选靶点鉴定库 细胞周期化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BMS-3 1338247-30-5 Cell Cycle/Checkpoint LIM Kinase BMS 3 inhibit Inhibitor LIMKs BMS3 LIM Kinase (LIMK) inhibitor

 

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