901245-65-6

901245-65-6 structure

Name: GSK 5959
Chemical Name: N-[1,3-Dimethyl-2-oxo-6-(1-piperidinyl)-2,3-dihydro-1H-benzimidazol-5-yl]-2-methoxybenzamide
CAS Number: 901245-65-6
Molecular Formula: C₂₂H₂₆N₄O₃
Molecular Weight: 394.467
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-04-18 08:15:22
Modify Date: 2024-01-02 16:56:22
GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.IC50 value: 80 nMTarget: BRPF1in vitro: GSK-5959 inhibits BRPF1 interaction with histone H3. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3 is employed to demonstrate GSK-5959 is cell permeability and disruption of chromatin binding with IC50 of 0.98 μM. GSK-5959 is used at 10 μM final concentration in various in vitro assays.

Name	N-[1,3-Dimethyl-2-oxo-6-(1-piperidinyl)-2,3-dihydro-1H-benzimidazol-5-yl]-2-methoxybenzamide
Synonyms	N-[1,3-Dimethyl-2-oxo-6-(1-piperidinyl)-2,3-dihydro-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- GSK 5959 GSK-5959

Description	GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.IC50 value: 80 nMTarget: BRPF1in vitro: GSK-5959 inhibits BRPF1 interaction with histone H3. A cellular protein interaction assay measuring the displacement of NanoLuc-tagged BRPF1 bromodomain from Halotagged histone H3 is employed to demonstrate GSK-5959 is cell permeability and disruption of chromatin binding with IC50 of 0.98 μM. GSK-5959 is used at 10 μM final concentration in various in vitro assays.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
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.