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

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

密度 

1.42±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

H2O: 7.3 mg/mL

形态

solid

酸度系数(pKa)

7.90±0.60(Predicted)

颜色

orange to red

生物活性

Ro 31-8220 是一种有效的 PKC 抑制剂，对 PKCα，PKCβI，PKCβII，PKCγ，PKCε 和大鼠大脑 PKC 的 IC50 值为 5，24，14，27，24 和 23 nM，同时能够有效抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β (IC50，3，8，15，38 nM), 对 MKK3，MKK4，MKK6 和 MKK7 无作用。

靶点

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 )

PKC-α 5 nM (IC 50 )

PKC-βII 14 nM (IC 50 )

体外研究

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.

体内研究

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.

WGK Germany 

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