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Cat. No. Name Size Price Add Cart
KI2072GSK 1210151A (I-BET151)5 mg$316
GSK 1210151A (I-BET151)10 mg$496
GSK 1210151A (I-BET151)25 mg$992
GSK 1210151A (I-BET151)100 mg$2032

Chemical Characteristic

Product NameGSK 1210151A (I-BET151)
SynonymsGSK1210151A
CAS No.1300031-49-5
Molecular Weight 415.4
FormulaC23H21N5O3
Chemical Name7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one
Smilesn1cc2c(c3cc(c(cc13)c1c(noc1C)C)OC)n(c(=O)[nH]2)[C@H](C)c1ccccn1
Chemical Structure

Biological activities

GSK1210151A is a novel and selective inhibitor of the bromodomain and extra terminal (BET) family proteins. GSK1210151A inhibits BRD2, BRD3, and BRD4 with IC50s of 0.5, 0.25, and 0.79 μM, respectively. GSK1210151A induces early cell cycle arrest and apoptosis and shows profound efficacy in human and murine MLL-fusion leukaemic cell lines. In vitro, GSK1210151A selectively and potently inhibits MLL-fusion leukaemic cell lines (including MV4;11, RS4;11, MOLM13, and NOMO1 cells) with IC50s ranging from 15 to 192 nM.[1] In a murine in vivo endotoxaemia model, GSK1210151A efficiently suppresses bacterial induced inflammation and sepsis.[2]

Protocols

In vitro: GSK1210151A is dissolved in DMSO.[1]

References

[1] Dawson MA, et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011, 478(7370): 529-533.
[2] Seal J, et al. Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012, 22(8): 2968-2972.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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