Ro 31-8220 formic is a potentPKCinhibitor, withIC50s of 5, 24, 14, 27, 24 and 23 nM forPKCα, PKCβI, PKCβII,PKCγ,PKCεand rat brainPKC, respectively. Ro 31-8220 formic also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Ro 31-8220 formic can also inhibit the expression of MKP-1, induce the expression ofc-Jun, and activateJNK, and these effects possess pharmacological properties independent ofPKC[1][2][3][4][5].
References:
[1].Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7.
Ro 31-8220 formic 是一种有效的PKC抑制剂，抑制PKCα，PKCβI，PKCβII，PKCγ，PKCε和大鼠大脑PKC的IC50值为 5，24，14，27，24 和 23 nM。Ro 31-8220 formic 也可抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β，IC50为 3，8，15，38 nM。Ro 31-8220 formic 还能抑制 MKP-1 的表达、诱导c-Jun表达并激活JNK，且这些作用存在不依赖于PKC的药理特性。