ro 32 0432

Ro 32-0432 is a selective, ATP-competitive, orally active pan-PKC inhibitor exhibiting inhibitory effects on PKCα, PKCβI, PKCβII, PKCγ, and PKCε. It blocks T-cell activation and may be employed in inflammatory and immune disorders. (S)-Ro 32-0432 hydrochloride is a GRK5 (G protein-coupled receptor kinase 5) inhibitor that alleviates nicotine withdrawal symptoms.

(S)-Ro 32-0432 is a potent, selective inhibitor of protein kinase C (PKC) and G protein-coupled receptor kinase 5 (GRK5), demonstrating ATP-competitive and oral activity. It presents IC50 values of 9.3 nM for PKCα, 28 nM for PKCβI, 30 nM for PKCβII, 36.5 nM for PKCγ, and 108.3 nM for PKCε, showcasing its effectiveness against multiple PKC isoforms. Additionally, (S)-Ro 32-0432 inhibits T-cell activation, indicating its potential application in the research of chronic inflammatory and autoimmune diseases [1] [2].

Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is an orally active pan-PKC inhibitor that inhibits PKCα, PKCβI, PKCβII, and PKCγ (IC50 = 9/28/31/37/108 nM).