cLIMK1i | LIMK1 inhibitor | Probechem Biochemicals

Chemical Structure : cLIMK1i

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cLIMK1i (Covalent inhibitor of LIMK1)

货号: PC-27241Not For Human Use, Lab Use Only.

cLIMK1i (Covalent inhibitor of LIMK1) is a potent, highly selective, irreversible covalent inhibitor of LIM domain kinase 1 (LIMK1) with biochemical IC50 of 25.6 nM, has 206-fold selectivity for inhibition of LIMK1 over LIMK2.

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生物&药学活性

cLIMK1i (Covalent inhibitor of LIMK1) is a potent, highly selective, irreversible covalent inhibitor of LIM domain kinase 1 (LIMK1) with biochemical IC50 of 25.6 nM, has 206-fold selectivity for inhibition of LIMK1 over LIMK2.
cLIMK1i is a type I inhibitor occupying the ATP-binding site with its acrylamide moiety oriented toward the P-loop where C349 resides.
cLIMK1i also has IC50 of 896 nM in HEK293T cellular assay when overexpressing either LIMK1 or LIMK2 and measuring downstream cofilin-1 phosphorylation, shows high selectivity for inhibition of LIMK1 over LIMK2.
cLIMK1i is an irreversible covalent LIMK1 inhibitor which binds LIMK1-C349.
cLIMK1i also has excellent kinome-wide selectivity.

物理化学性质&存储条件

分子量	398.39
分子式	C21H17F3N4O
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	N-(3'-methyl-5'-((4-(trifluoromethyl)pyrimidin-2-yl)amino)-[1,1'-biphenyl]-4-yl)acrylamide

参考文献

1. Patteson JB, et al. J Biol Chem. 2026 Jul 13:113322. doi: 10.1016/j.jbc.2026.113322.

cLIMK1i (Covalent inhibitor of LIMK1)

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物理化学性质&存储条件

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cLIMK1i (Covalent inhibitor of LIMK1)

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