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GSK9311

Names

[ CAS No. ]:
1923851-49-3

[ Name ]:
GSK9311

Biological Activity

[Description]:

GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Research Areas >> Cancer

[Target]

IC50: 6.0 (BRPF1), 4.3 (BRPF2)[1]


[In Vitro]

GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrates properties suitable for cellular and in vivo studies. GSK6853 is a less active analogue of GSK6853 in which the 5-amide is alkylated[1].

[References]

[1]. Bamborough P, et al. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain. ACS Med Chem Lett. 2016 May 9;7(6):552-7.


[Related Small Molecules]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15

Chemical & Physical Properties

[ Molecular Formula ]:
C24H31N5O3

[ Molecular Weight ]:
437.544


Related Compounds

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