1G,10G,100G,1KG
| 中文名称 | 1G,10G,100G,1KG |
|---|---|
| 中文同义词 | RO31-8220甲磺酸盐是广谱PKC抑制剂;化合物 T6643L |
| 英文名称 | RO 31-8220 METHANESULFONATE |
| 英文同义词 | BISINDOLYLMALEIMIDE IX METHANESULFONATE;BISINDOYLMALEIMIDINE IX METHANESULFONATE;RO-31-8220;RO 31-8220 MESYLATE;RO 31-8220 METHANESULFONATE;3-[3-[2,5-DIHYDRO-4-(1-METHYL-1H-INDOL-3-YL)-2,5-DIOXO-1H-PYRROL-3-YL]-1H-INDOL-1-YL]PROPYL CARBAMIMIDOTHIOIC ACID ESTER MESYLATE;3-[1-3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL) MALEIMIDE;3-[1-[3-(AMIDINOTHIO)PROPYL-1H-INDOL-3-YL]-3-(1-METHYL-1H-INDOL-3-YL)MALEIMIDE METHANESULFONATE |
| CAS号 | 125314-64-9 |
| 分子式 | C25H23N5O2S |
| 分子量 | 457.55 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;Protein Kinase |
| Mol文件 | 125314-64-9.mol |
| 结构式 |  |
1G,10G,100G,1KG 性质
| 密度 | 1.42±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | H2O: 7.3 mg/mL |
| 酸度系数(pKa) | 7.90±0.60(Predicted) |
| 形态 | 固体 |
| 颜色 | 橙色至红色 |
|
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.
安全信息
| WGK Germany | 3 |
|---|
| 提供商 | 语言 |
|---|---|
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英文
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| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-13866 | Ro 31-8220 mesylate | 5 mg | 801元 | |
| 2024/04/30 | HY-13866 | 1G,10G,100G,1KG Ro 31-8220 mesylate | 125314-64-9 | 10 mg | 1244元 |