Description
GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
Product information
CAS Number: 1923851-49-3
Molecular Weight: 437.53
Formula: C24H31N5O3
Chemical Name: N-{1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxo-2,3-dihydro-1H-1,3-benzodiazol-5-yl}-N-ethyl-2-methoxybenzamide
Smiles: CCN(C(=O)C1=CC=CC=C1OC)C1C=C2C(=CC=1N1CCNC[C@H]1C)N(C)C(=O)N2C
InChiKey: WFXIHQFRQPGCCR-MRXNPFEDSA-N
InChi: InChI=1S/C24H31N5O3/c1-6-28(23(30)17-9-7-8-10-22(17)32-5)20-13-18-19(27(4)24(31)26(18)3)14-21(20)29-12-11-25-15-16(29)2/h7-10,13-14,16,25H,6,11-12,15H2,1-5H3/t16-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (228.56 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
References:
- 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.
Products are for research use only. Not for human use.
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