Cayman BIX 02565

The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC₅₀ value of 1.1 nM.^, It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC₅₀s = 0.052-1.820 μM for adrenergic α_1A, α_1B, α_1D, α_2A, β₂, and imidazoline I₂ receptors.^, BIX 02565 can also inhibit LRRK2 and PRKD1 with IC₅₀ values of 16 and 35 nM, respectively). In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.

WARNING This product is not for human or veterinary use.