WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406745
CAS#: 1910124-24-1
Description: GSK6853 is a potent (300 pM), soluble, cell active (20 nM), and highly selective inhibitor of the BRPF1 bromodomain, and demonstrated properties suitable for cellular and in vivo studies. The BRPF (Bromodomain and PHD Fingercontaining) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. BRPF1 (bromodomain and PHD finger containing protein 1) is involved in the epigenetic regulation of gene expression and have been implicated in human cancer.
Hodoodo Cat#: H406745
Name: GSK6853
CAS#: 1910124-24-1
Chemical Formula: C22H27N5O3
Exact Mass: 409.21
Molecular Weight: 409.490
Elemental Analysis: C, 64.53; H, 6.65; N, 17.10; O, 11.72
Synonym: GSK6853; GSK 6853; GSK-6853.
IUPAC/Chemical Name: (R)-N-(1,3-dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
InChi Key: FQWDVNSBYDXPIO-CQSZACIVSA-N
InChi Code: InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1
SMILES Code: O=C(NC1=C(N2[C@H](C)CNCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
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The following data is based on the product molecular weight 409.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
Paul Bamborough, Heather A. Barnett, Isabelle Becher, Mark J. Bird, Chun-wa Chung, Peter D. Craggs, Emmanuel H. Demont, Hawa Diallo, David J. Fallon, Laurie J. Gordon, Paola Grandi, Clare I. Hobbs, Edward Hooper-Greenhill, Emma J. Jones, Robert P. Law, Armelle Le Gall, David Lugo, Anne-Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Robert J. Sheppard, Allan J. B. Watson, and Robert J. Watson
Publication Date (Web): May 9, 2016 (Featured Letter)
DOI: 10.1021/acsmedchemlett.6b00092