BIX 02565

SKU: orb1220996

Description

BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2 IC50: 1.1 nM).

Key Properties

• CAS Number: 1311367-27-7
• MW: 458.56
• Purity: >98% (HPLC)
• Formula: C₂₆H₃₀N₆O₂
• SMILES: C[C@@H]1CCNC(=O)c2cc3ccc(cc3n12)C(=O)Nc1nc2ccccc2n1CCCN(C)C
• Target: S6 Kinase
• Solubility: DMSO: 20 mg/mL

Bioactivity

• 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.
• In Vitro:
  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. BIX 02565, a second Rsk inhibitor, protects enzyme active sites from reaction with biotinylated nucleotide acyl phosphates.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

S6 Kinase