145317-11-9

Ro 31-8425 (145317-11-9) is a selective, reversible, ATP-competitive inhibitor of protein kinase C. Inhibits PKCα, β1, β2, γ and ε, IC50= 8, 8, 14,13 and 39 nM respectively.1? Extremely useful tool for probing PKC-dependent physiology2 or signaling pathways3. Increases MSC adhesion to an ICAM-1 coated substrate in vitro and enables targeted delivery of systematically administered MSCs to inflamed sites in vivo in a CD11a-dependent manner.4? Cell permeable.

Bisindolylmaleimide X hydrochloride is a potent and selective cell-permeable protein kinase C (PKC) inhibitor. Studies reveal that inhibition of PKCα by Bisindolylmaleimide X and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure.

PKC; CDK2: 200 nM (IC₅₀)

1) Wilkinson et al. (1993), Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C; Biochem. J., 294 335 2) Niu et al. (2011), PKCε regulates contraction-stimulated GLUT4 traffic in skeletal muscle cells; J. Cell Physiol., 226 173 3) Jimenez-Lopez et al. (2005), Protein kinase C signaling as a survival pathway against CYP2E1-derived oxidative stress and toxicity in HepG2 cells; J. Pharmacol. Exp. Ther., 312 998 4) Levy et al. (2015), A small-molecule screen for enhanced homing of systemically infused cells; Cell Rep., 10 1261