RO-31-8220

RO-31-8220化学性质

储存条件 :2-8°C
溶解度 :DMSO:52.77(Max Conc. mg/mL);95.31(Max Conc. mM)
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)
形态 :Red solid
颜色 :Red

安全信息

RO-31-8220性质、用途与生产工艺

生物活性 Ro 31-8220 mesylate 是一种有效的 PKC 抑制剂，抑制 PKCα，PKCβI，PKCβII，PKCγ，PKCε 和大鼠大脑 PKC 的 IC50 值为 5，24，14，27，24 和 23 nM，也可抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β，IC50为3，8，15，38 nM。

靶点

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 )

体外研究

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.
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.

RO-31-8220上下游产品信息

上游原料

下游产品

RO-31-8220生产厂家

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