Ro 31-8220 is a potent inhibitor of PKC with IC50 values 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 IC50 values of 3, 8, 15, and 38 nM, respectively, without affecting MKK3, MKK4, MKK6, and MKK7.

Ro 31-8220 is a potent inhibitor of protein kinase C (PKC), with IC50 values of 5, 24, 14, 27, 24, and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, respectively. It also inhibits MAPKAP-K1b, MSK1, S6K1, and GSK3β with IC50 values of 3, 8, 15, and 38 nM, while showing no effect on MKK3, MKK4, MKK6, and MKK7. Additionally, Ro 31-8220 directly suppresses voltage-dependent Na+ channels and provides neuroprotection against paraoxon-induced neuronal cell death in cerebellar granule neurons by inhibiting paraoxon-induced caspase-3 activity and reducing increased phospho-PKC pan levels at a concentration of 1μM.

Ro 31-8220, administered subcutaneously at a dosage of 6 mg/kg/day, is well-tolerated in mice with a half-life of 5.7 hours. Treatment with Ro 31-8220 significantly improves fractional shortening in MLP/mice over a period of 6 weeks, whereas there is no observable effect in wild-type (WT) mice [4].