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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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