1H-Pyrrole-2,5-dione, 3-[8-(aMinoMethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-Methyl-1H-indol-3-yl)-, Monohy

Description

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.

Uses

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.

References

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