GSK-5959 MedChemExpress (MCE)

Product Name	GSK-5959
Synonyms	CS-1636 GSK5959 GSK-5959 BRPF1-IN-3 N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide Benzamide, N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxy-
CAS	901245-65-6
EINECS
Chemical Formula	C22H26N4O3
Molecular Weight	394.47
inchi
Package	10 mM * 1 mL;5 mg;10 mg;50 mg
Price	Email to quote
Descriptions	GSK-5959 GSK-5959 MedChemExpress (MCE) HY-18665 901245-65-6 98.74% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions GSK-5959 GSK-5959 MedChemExpress (MCE) HY-18665 901245-65-6 98.74% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with an IC50 of ~ 80 nM. GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold)[2]. GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay[2]. GSK-5959 has no effect on TRIM24 SUMOylation[3]. IC50: 80 nM (BRPF1)[1]. Cellular Effect Cell Line Type Value Description References \| \| \| \| \| \| \| \| \| \| [1]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195. [Content Brief] [2]. Wylie S.Palmer, et al. Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains Discovery Today: Technologies Volume 19, March 2016, Pages 65-71. [3]. Srikanth Appikonda, et al. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesionJ Biol Chem. 2018 May 11 293(19):7476-7485. [Content Brief]
Supplier Website	https://www.medchemexpress.com/GSK-5959.html
Last Update	2025-04-01 14:45:47

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