Ro 31-8220 Mesylate

Ro 31-8220 Mesylate是一种蛋白激酶C(PKC)的选择性抑制剂,对PKC α\PKC βI\PKC βII\PKC γ和PKC ε的IC50值分别为5\24\14\27和24 nM[1].

PKC是一种单体的Ca2+和磷脂依赖的Ser/Thr蛋白激酶,在生长因子激活的信号通路和恶性转化中扮演重要角色[1].

Ro 31-8220 Mesylate是一种PKC的选择性抑制剂.另外,Ro 31-8220可提高生长因子刺激的c-Jun表达,但抑制MKP-1和c-Fos表达.Ro-31-8220可以PKC依赖的方式强力地刺激应力活化的蛋白激酶JNK1[2].在外周血单核细胞中,Ro 31-8220可抑制有丝分裂原诱导的白细胞介素(IL)-2生成和IL-2依赖的T淋巴母细胞增殖,IC50值分别为80和350 nM.另外,Ro 31-8220(400 nM)可抑制27%的IL-2Rα(CD25)表达,表明Ro 31-8220可抑制早期和晚期T细胞活化[3].

在大鼠脂肪细胞和L6肌小管中,RO 31-8220可活化c-Jun N端激酶(JNK)和糖原合酶(GS),并可刺激葡萄糖并入糖原.RO 31-8220可以PKC依赖的方式抑制胞外响应激酶1和2(ERK1/2)活性[4].

参考文献：
[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.