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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Focal Adhesion Kinase (FAK)-M64HCl
M64HCl

Chemical Structure : M64HCl

CAS No.: 2769848-56-6

M64HCl (M64 hydrochloride)

货号: PC-22945Not For Human Use, Lab Use Only.

M64HCl is a specific small molecule, water-soluble focal adhesion kinase (FAK) activator, interacts directly with the FAK kinase domain to activate FAK, induces epithelial sheet migration in vitro, and stimulates gut mucosal wound healing in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

M64HCl is a specific small molecule, water-soluble focal adhesion kinase (FAK) activator, interacts directly with the FAK kinase domain to activate FAK, induces epithelial sheet migration in vitro, and stimulates gut mucosal wound healing in vivo.
M64HCl activates FAK-Tyr397 phosphorylation at 100 pM and 1 ​nM by 8.7 ​± ​3.0%, 9.1 ​± ​3.9% respectively in Caco-2 ​cells.
M64HCl increases FAK-Tyr-397 phosphorylation in comparison to H2O controls by 20.2 ​± ​7.4% at 100 ​nM.
M64HCl does not activate the FAK paralog, proline-rich tyrosine kinase 2 (Pyk2), and non-receptor protein tyrosine kinase Src.
M64HCl not only activates FAK but also stimulates epithelial sheet migration.
M64HCl dose-responsively activates the FAK kinase domain vs. the non-salt M64, increasing the Vmax of ATP-binding.
M64HCl (25 ​mg/kg/day) promotes mucosal healing in two murine small intestinal injury models.

物理化学性质&存储条件

分子量 473.93
分子式 C21H27ClF3N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(2-(dimethylamino)-2-(pyridin-4-yl)ethyl)-3-(2-morpholino-5-(trifluoromethyl)phenyl)urea hydrochloride

参考文献

1. Wang Q, et al. Curr Res Pharmacol Drug Discov. 2022 Dec 23;4:100147.

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