125314-64-9
125314-64-9 结构式
基本信息
RO 31-8220 MESYLATE
BisindolylMaleiMide IX
Bisindoylmaleimidine IX
RO 31-8220 METHANESULFONATE
Ro 31-8220 methanesulfonate salt
BISINDOLYLMALEIMIDE IX METHANESULFONATE
BISINDOYLMALEIMIDINE IX METHANESULFONATE
Ro 31-8220 mesylate (Bisindolylmaleimide IX)
3-[1-3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL) MALEIMIDE
物理化学性质
常见问题列表
|
PKC-α 5 nM (IC 50 ) |
PKC-βII 14 nM (IC 50 ) |
PKC-βI 24 nM (IC 50 ) |
PKC-ε 24 nM (IC 50 ) |
PKC-γ 27 nM (IC 50 ) |
Rat Brain PKC 23 nM (IC 50 ) |
MAPKAP-K1b 3 nM (IC 50 ) |
MSK1 8 nM (IC 50 ) |
S6K1 15 nM (IC 50 ) |
GSK3β 38 nM (IC 50 ) |
Ro 31-8220 is a potent PKC inhibitor, with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC 50 s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na + channels. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels.
Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP −/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change.