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BIX 02565

Chemical Structure : BIX 02565

CAS No.: 1311367-27-7

BIX 02565 (BIX02565 )

Catalog No.: PC-21764Not For Human Use, Lab Use Only.

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

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 458.57
Formula C26H30N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5R)-N-[1-[3-(Dimethylamino)propyl]-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-5-methyl-1-oxo-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide

References

1. Thomas M Kirrane, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42.

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