Uses
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.
General Description
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.
