Chemical Name:3-[3-[2,5-Dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-
1H-pyrrol-3-yl]-1H-indol-1-yl]propyl carbamimidothioic
acid ester mesylate
Biological Activity:
Protein
kinase C inhibitor, with activity at other protein kinases (IC50
values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively). Activates
JNK and glycogen synthase, and inhibits MAPK and ERK2, in rat adipocytes and L6
myotubes. Also inhibits voltage-dependent Na+ channels in the
micromolar range.
Daviset al (1989) Potent, selective inhibitors of protein
kinase C. FEBS Lett. 259 61. Standaertet al (1999)
RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in
rat adipocytes and L6 myotubes. Comparison to actions of insulin. Endocrinol. 150
2145. Lingameneniet al (2000) Inhibition of voltage-dependent
sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS
Lett. 473 265. Davieset al (2000) Specificity and
mechanism of action of some commonly used protein kinase inhibitors. Biochem.J.
351 95.