BIX 02565 is a potent, selective ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.
BIX 02565 is 100-fold selective relative to RSK for a kinase panel, with the exception of LRRK2 and PRKD1, for which showed 16- and 35-fold selectivity.
BIX 02565 (1, 3, and 10 mg/kg) in the rat CV screen resulted in a precipitous decrease in both mean arterial pressure (MAP; to -65 ± 6 mm Hg below baseline) and heart rate (-93 ± 13 beats/min).
BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicited concentration-dependent decreases in MAP in telemetry-instrumented rats.
