RO-31-8220
| 中文名称 | RO-31-8220 |
|---|---|
| 中文同义词 | 双吲哚马来酰亚胺 IX 甲烷磺酸盐;RO31-8220 MSOH盐;MK-7123, PS-291822;3-(3-(4-(1-甲基-1H-吲哚-3-基)-2,5-二氧代-2,5-二氢-1H-吡咯-3-基)-1H-吲哚-1-基)丙基异硫脲甲磺酸盐;RO 31-8220 甲磺酸盐;RO 31-8220 (PKC抑制剂) |
| 英文名称 | RO-31-8220 |
| 英文同义词 | RO-31-8220;BISINDOLYLMALEIMIDE IX, METHANESULFONATE;3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE;BISINDOLYLMALEIMIDE IX METHANESULPHONATE SALT;BisindolylMaleiMide IX Mesylate;BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220];Carbamimidothioic acid, 3-[3-[2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl ester, methanesulfonate (1:1);Ro31-8220MsOH |
| CAS号 | 138489-18-6 |
| 分子式 | C25H23N5O2S |
| 分子量 | 457.55 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;抑制剂;Smad;TGF-beta;Inhibitors;inhibitor;TGF-beta/Smad |
| Mol文件 | 138489-18-6.mol |
| 结构式 |  |
RO-31-8220 性质
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | DMSO:52.77(最大浓度 mg/mL);95.31(最大浓度 mM) DMF:25.0(最大浓度 mg/mL);45.15(最大浓度 mM) DMF:PBS ( pH 7.2) (1:9):0.1(最大浓度 mg/mL);0.18(最大浓度 mM) 乙醇:2.77(最大浓度 mg/mL);5.0(最大浓度 mM) |
| 形态 | 红色固体 |
| 颜色 | 红色 |
|
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.
安全信息
| 海关编码 | 2933790090 |
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