138489-18-6
138489-18-6 结构式
基本信息
双吲哚马来酰亚胺 IX 甲烷磺酸盐
MK-7123, PS-291822
RO-31-8220
Ro31-8220MsOH
Ro 31-8220 Mesylat
Ro 31-8220/Ro318220
RO-31-8220 USP/EP/BP
BisindolylMaleiMide IX Mesylate
BISINDOLYLMALEIMIDE IX, METHANESULFONATE
Ro-31-8220 - CAS 138489-18-6 - Calbiochem
Bisindolylmaleimide IX (Ro 31-8220 Mesylate)
物理化学性质
DMF:25.0(Max Conc. mg/mL);45.15(Max Conc. mM)
DMF:PBS (pH 7.2) (1:9):0.1(Max Conc. mg/mL);0.18(Max Conc. mM)
Ethanol:2.77(Max Conc. mg/mL);5.0(Max Conc. mM)
常见问题列表
|
PKC-α 5 nM (IC 50 ) |
PKC-βI 24 nM (IC 50 ) |
PKC-βII 14 nM (IC 50 ) |
PKC-γ 27 nM (IC 50 ) |
PKC-ε 24 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 mesylate 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.