RO-32-0432

The Uses of RO-32-0432

Bisindolylmaleimide XI is a potent and selective cell-permeable protein kinase C (PKC) inhibitor. Studies reveal that inhibition of PKCα by Bisindolylmaleimide XI and other similar PKC inhibitors has been associated with enhanced cardiac contractility and protection from heart failure. Bisindolylmaleimide XI has been shown to prevent T-cell activation and proliferation associated with chronic infl ammatory responses in vivo.

Biological Activity

Selective cell-permeable protein kinase C inhibitor. Displays slight selectivity for conventional PKC isoforms over Ca 2+ and atypical PKC isoforms; binding affinities for rat isoforms are 9, 28, 31, 37 and 108 nM for PKC's α , β Ι, β ΙΙ, γ and ε respectively. Orally available and prevents T-cell chronic inflammation in vivo .