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Description

A cell permeable bis-aryl urea that acts as a highly potent and selective LIMK inhibitor (LIM kinase, IC50 = 43 nM for Limk1) with more than 400-fold selectivity against ROCK and JNK kinases. Only displays inhibitory effect on STK16 with >=80% inhibition at 1 µ,M in addition to LIMK1 in a 61 kinase panel profiling. Inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM), PC-3 and CEM-SS T cells (IC50<1 µ,M), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µ,M. Exhibits desirable pharmacokinetic properties in vitro and in vivo with 36% bioavailability in rats (p.o. at 2mg/kg)., A cell permeable bis-aryl urea that acts as a highly potent and selective LIMK inhibitor (LIM kinase, IC50 = 43 nM for Limk1) with more than 400-fold selectivity against ROCK and JNK kinases. Only displays inhibitory effect on STK16 with >=80% inhibition at 1 µ,M in addition to LIMK1 in a 61 kinase panel profiling. Inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM), PC-3 and CEM-SS T cells (IC50<1 µ,M), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µ,M. Exhibits desirable pharmacokinetic properties in vitro and in vivo with 36% bioavailability in rats (p.o. at 2mg/kg).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.