General description

Feng, Y., et al. 2008. J. Med. Chem.51, 6642.

A cell-permeable pyrazolyl carboxamide compound that acts as a potent, ATP-binding pocket-targeting inhibitor of ROCK-II (IC₅₀ = 1.5 nM) and effectively inhibits the myosin light chain 2 phosphorylation on Thr18/Ser19 in A7r5 cells (IC₅₀ = 72 nM). It afftects the activities of PKA, MRCK, Akt1 (IC₅₀ = 0.186, 1.19, and 1.41 µM, respectively) and CYP-450 enzymes (% inhibition of 2C9/2D6/3A4/1A2 at 10 µM = 87/40/1/20, respectively) only at much higher concentrations.

Legal Information

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

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

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)