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。
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.