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。Ro 31-8220还显著抑制 MAPKAP-K1b，MSK1，S6K1 和 GSK3β，IC50值分别为3，8，15，38 nM，对 MKK3，MKK4，MKK6 和 MKK7 无作用。

Ro 31-8220 is a potent inhibitor of PKC 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 with IC50s of 3, 8, 15, and 38 nM, respectively without effect on MKK3, MKK4, MKK6 and MKK7.

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 [1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC 50 s, 3, 8, 15, and 38 nM, respectively), without effect on MKK3, MKK4, MKK6 and MKK7. Furthermore, Ro 31-8220 directly suppresses voltage-dependent Na + channels [2]. 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 [3].

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 significant rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change [4].

125314-64-9

C25H23N5O2S

457.55

Ro 31-8220

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years