Ro 31-8220 methanesulfonate

Uses

Ro 31-8220 Mesylate is a protein kinase C (PKC) inhibitor.

Definition

ChEBI: Ro 31-8220 is an imidothiocarbamic ester, a member of indoles and a member of maleimides. It has a role as an EC 2.7.11.13 (protein kinase C) inhibitor. It is functionally related to a maleimide.

Biological Activity

Protein kinase C inhibitor, with activity at other protein kinases (IC 50 values are 33, 3, 8, 15 and 38 nM for PKC α , MAPKAP-K1b, MSK1, GSK3 β 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.

in vivo

IC 50

PKC-α: 5 nM (IC₅₀); PKC-βII: 14 nM (IC₅₀); PKC-βI: 24 nM (IC₅₀); PKC-ε: 24 nM (IC₅₀); PKC-γ: 27 nM (IC₅₀); Rat Brain PKC: 23 nM (IC₅₀); MAPKAP-K1b: 3 nM (IC₅₀); MSK1: 8 nM (IC₅₀); S6K1: 15 nM (IC₅₀); GSK3β: 38 nM (IC₅₀)

References

[1]. wilkinson se, parker pj, nixon js. isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase c. biochem j, 1993, 294 ( pt 2): 335-337.
[2]. beltman j, mccormick f, cook sj. the selective protein kinase c inhibitor, ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (mkp-1) expression, induces c-jun expression, and activates jun n-terminal kinase. j biol chem, 1996, 271(43): 27018-27024.
[3]. geiselhart l, conti dj, freed bm. ro 31-8220, a novel protein kinase c inhibitor, inhibits early and late t cell activation events. transplantation, 1996, 61(11): 1637-1642.
[4]. standaert ml, bandyopadhyay g, antwi ek, et al. ro 31-8220 activates c-jun n-terminal kinase and glycogen synthase in rat adipocytes and l6 myotubes. comparison to actions of insulin.