Lim Kinase Inhibitor II; SR- 1PC X 5MG

Biochem/physiol Actions

Reversible: yes

Primary TargetLIMK

Cell permeable: yes

General 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 µM 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 µM), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µM. 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 µM 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 µM), shown to inhibit cell invasion by 76% and cell migration by 74% in PC-3 cells at 1 µM. 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Yin, Y., et al. 2015. J. Med. Chem.58, 1846.

Packaging

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C

Warning

Toxicity: Standard Handling (A)