| Bioactivity | BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM. | ||||||||||||
| Target | IC50: 1.1 nM (RSK2) | ||||||||||||
| Invitro | BIX 02565, a potent RSK2 inhibitor (IC50=1.1 nM) targets for the treatment of heart failure secondary to myocardial infarction through indirect NHE inhibition[1]. BIX 02565, a second Rsk inhibitor, protects enzyme active sites from reaction with biotinylated nucleotide acyl phosphates[2]. | ||||||||||||
| In Vivo | In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicits concentration-dependent decreases in MAP after each dose (to -39±4 mm Hg on day 4 at Tmax). BIX 02565 produces concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring at concentrations above 0.03 μM with a calculated EC50 of 3.1 μM. Subsequently, BIX 02565 is infused in the anesthetized rat in a low-dose (0.1, 0.3, and 1.0 mg/kg per 20 min) and high-dose (1.0, 3.0, and 10.0 mg/kg per 20 min) series of continuous infusions to test the effect of compound on hemodynamics in vivo[1]. | ||||||||||||
| Name | BIX 02565 | ||||||||||||
| CAS | 1311367-27-7 | ||||||||||||
| Formula | C26H30N6O2 | ||||||||||||
| Molar Mass | 458.56 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Fryer RM, et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. Journal of Pharmacology and Experimental Therapeutics (2012), 340(3), 492-500. [2]. Edgar AJ, et al. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2013 Dec 17. |