Chemical Structure : cLIMK1i
CAS No.:
cLIMK1i
(Covalent inhibitor of LIMK1)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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398.39
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Formula
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C21H17F3N4O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(3'-methyl-5'-((4-(trifluoromethyl)pyrimidin-2-yl)amino)-[1,1'-biphenyl]-4-yl)acrylamide
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References
1. Patteson JB, et al. J Biol Chem. 2026 Jul 13:113322. doi: 10.1016/j.jbc.2026.113322.
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