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BMS-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-3图片
CAS NO:1338247-30-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
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产品介绍
理化性质和储存条件
Molecular Weight (MW) 429.27
Formula C17H12Cl2F2N4OS
CAS No. 1338247-30-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) O=C(C1CC1)NC2=NC=C(C3=CC(C(F)F)=NN3C4=C(Cl)C=CC=C4Cl)S2
Synonyms BMS-3; BMS 3; BMS3.

Chemical Name: N-[5-[2-(2,6-Dichlorophenyl)-5-(difluoromethyl)pyrazol-3-yl]-1,3-thiazol-2-yl]cyclopropanecarboxamide

InChi Key: YBGGBHCJSAEIAS-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H12Cl2F2N4OS/c18-9-2-1-3-10(19)14(9)25-12(6-11(24-25)15(20)21)13-7-22-17(27-13)23-16(26)8-4-5-8/h1-3,6-8,15H,4-5H2,(H,22,23,26)

SMILES Code: O=C(C1CC1)NC2=NC=C(C3=CC(C(F)F)=NN3C4=C(Cl)C=CC=C4Cl)S2

实验参考方法
In Vitro

In vitro activity: BMS-3 is a potent inhibitor of the LIM kinase (LIMK)with IC50 of 5nM and 6 nM for LIMK1 and LIMK2 respectively. Inhibition of LIMK1 by specific inhibitors (BMS-3) resulted in lower levels of actin polymerization during capacitation and a dramatic decrease in the percentage of sperm that undergo acrosomal exocytosis. Thus, we demonstrated for the first time that the master regulators of actin dynamics in somatic cells are present and active in mouse sperm. Combining the results of our present study with other results from the literature, we have proposed a working model regarding how LIMK1 and Cofilin control acrosomal exocytosis in mouse sperm.


Kinase Assay: 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).


Cell Assay: 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.

In VivoMouse 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.
Animal model
Formulation & Dosage
References Mol Cancer Ther. 2008 Nov;7(11):3490-8; Dev Biol. 2015 Sep 15;405(2):237-49.