产品描述:
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.{30925,30924} 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 α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.{30925,30924} BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).{30925} In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.{30924}