LIM KINASE INHIBITOR II SR-7826 (C15-1305-353)

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
LIMK

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 387.43. Empirical Formula: C₂₂H₂₁N₅O₂. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.