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BMS-5

BMS-5

产品编号 T4598   CAS 1338247-35-0
别名: BMS5, LIMKi 3

BMS-5 (LIMKi 3) 是一种有效的 LIMK 抑制剂,抑制LIMK1和LIMK2的IC50分别为 7 nM 和 8 nM。

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BMS-5 Chemical Structure
BMS-5, CAS 1338247-35-0
规格 价格/CNY 货期 数量
1 mg ¥ 293 现货
2 mg ¥ 432 现货
5 mg ¥ 652 现货
10 mg ¥ 985 现货
25 mg ¥ 1,390 现货
50 mg ¥ 2,190 现货
100 mg ¥ 3,270 现货
1 mL * 10 mM (in DMSO) ¥ 652 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: BMS-5 (T4598)
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纯度: 99.88%
纯度: 95.83%
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生物活性
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存储 & 溶解度
参考文献
产品描述 BMS-5 (LIMKi 3) is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
靶点活性 LIMK1:7 nM, LIMK2:8 nM
体外活性 BMS-5 inhibits cofilin-Ser3 phosphorylation in a dose-dependent manner in Nf2ΔEx2 mouse Schwann cells (MSCs) with an IC50 of ~2 μM. BMS-5 reduces Nf2ΔEx2 MSC viability in a dose-dependent manner with an IC50 of 3.9 μM, but does not significantly reduce the viability of control Nf2flox2/flox2 MSCs at equivalent BMS-5 concentrations. At 10 μM BMS-5, Nf2ΔEx2 MSC viability is 40% compared to 83% for controls[2] .
体内活性 BMS-5 (20 or 200 μM/side) is bilaterally infused into the hippocampus of rats immediately after contextual fear conditioning training. Rats are tested for memory consolidation 48 h after fear conditioning. Post hoc analysis shows that the group treated with 200 μM BMS-5 express lower freezing levels compared to the 20 μM and vehicle groups (P
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-5) 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]
细胞实验 Cell membrane asymmetry is measured. Nf2ΔEx2 MSCs plated in a 6-well format are incubated with 2 μM BMS-5 or DMSO vehicle for 24 hrs. Cell are harvested and assayed. Plasma membrane asymmetry is evaluated with the Violet ratiometric assay by flow cytometry[2] .
动物实验 Rats [3]
别名 BMS5, LIMKi 3
分子量 431.29
分子式 C17H14Cl2F2N4OS
CAS No. 1338247-35-0

存储

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

溶解度

DMSO: 55 mg/mL (127.52 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 2.3186 mL 11.5931 mL 23.1863 mL 57.9656 mL
5 mM 0.4637 mL 2.3186 mL 4.6373 mL 11.5931 mL
10 mM 0.2319 mL 1.1593 mL 2.3186 mL 5.7966 mL
20 mM 0.1159 mL 0.5797 mL 1.1593 mL 2.8983 mL
50 mM 0.0464 mL 0.2319 mL 0.4637 mL 1.1593 mL
100 mM 0.0232 mL 0.1159 mL 0.2319 mL 0.5797 mL

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TargetMol Library Books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. Petrilli A, et al. LIM Domain Kinases as Potential Therapeutic Targets for Neurofibromatosis Type 2.Oncogene. Oncogene. 2014 Jul 3;33(27):3571-82. 3. Lunardi P, et al. Effects of Hippocampal LIMK Inhibition on Memory Acquisition, Consolidation, Retrieval, Reconsolidation, and Extinction. Mol Neurobiol. 2017 Jan 13. 4. Gao T T, Wang Y, Liu L, et al. LIMK1/2 in the mPFC plays a role in chronic stress-induced depressive-like effects in mice[J]. International Journal of Neuropsychopharmacology. 2020, 23(12): 821-836.

TargetMol Library Books文献引用

1. Gao T T, Wang Y, Liu L, et al. LIMK1/2 in the mPFC plays a role in chronic stress-induced depressive-like effects in mice. International Journal of Neuropsychopharmacology. 2020, 23(12): 821-836.
LX7101 LY2812223 SM1-71 T56-LIMKi BMS-3 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:
激酶抑制剂库 抗癌化合物库 NO PAINS 化合物库 表型筛选靶点鉴定库

TargetMol Calculator剂量换算

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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。

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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-5 1338247-35-0 Cell Cycle/Checkpoint LIM Kinase LIMKi3 BMS5 inhibit LIM Kinase (LIMK) LIMKs Inhibitor BMS 5 LIMKi 3 LIMKi-3 inhibitor

 

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