1311367-27-7 Usage
Biological Activity
bix 02565 is a novel inhibitor of ribosomal s6 kinase 2 with ic50 value of 1 nm [1].ribosomal s6 kinase (rsk) is a na/h exchanger (nhe) -activating factor and is important for ph maintenance during the early phase of cellular stress. while, nhe activation leads to ca2+ overload and cardiac hypertrophy over longer periods [2].bix 02565 is a novel rsk2 inhibitor. also, bix 02565 inhibited adrenergic ɑ1a-, ɑ1b-, ɑ1d-, ɑ2a-, β2- and imidazoline i2 receptors with ic50 values ranging from 0.052 to 1.820 μm. these receptors played important roles in the regulation of vascular tone and cardiac function [2]. also, bix 02565 inhibited lrrk2 and prkd1 with ic50 values of 16 and 35 nm [1].in the rat cv screen, bix 02565 (1, 3 and 10 mg/kg) significantly decreased heart rate (-93 +13 beats/min) and mean arterial pressure (map: to -65 +6 mm hg below baseline). in telemetry-instrumented rats, bix 02565 (30, 100 and 300 mg/kg for 4 days) reduced map (to -39 + 4 mm hg) in a concentration-dependent way [2].
references
[1]. kirrane tm, boyer sj, burke j, et al. indole rsk inhibitors. part 2: optimization of cell potency and kinase selectivity. bioorg med chem lett, 2012, 22(1): 738-742. [2]. fryer rm, muthukumarana a, chen rr, et al. mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal s6 kinase 2 inhibitors. j pharmacol exp ther, 2012, 340(3): 492-500.
Check Digit Verification of cas no
The CAS Registry Mumber 1311367-27-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,1,1,3,6 and 7 respectively; the second part has 2 digits, 2 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1311367-27:
(9*1)+(8*3)+(7*1)+(6*1)+(5*3)+(4*6)+(3*7)+(2*2)+(1*7)=117
117 % 10 = 7
So 1311367-27-7 is a valid CAS Registry Number.
1311367-27-7Relevant articles and documents
HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE
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Page/Page column 13, (2011/06/26)
Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
