GSK 5959

Modify Date: 2024-01-02 16:56:22

GSK 5959 structure	Common Name	GSK 5959
	CAS Number	901245-65-6	Molecular Weight	394.467
	Density	1.3±0.1 g/cm3	Boiling Point	527.3±50.0 °C at 760 mmHg
	Molecular Formula	C₂₂H₂₆N₄O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	272.7±30.1 °C

Use of GSK 5959

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
Synonym	More Synonyms

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.

Density	1.3±0.1 g/cm3
Boiling Point	527.3±50.0 °C at 760 mmHg
Molecular Formula	C₂₂H₂₆N₄O₃
Molecular Weight	394.467
Flash Point	272.7±30.1 °C
Exact Mass	394.200500
LogP	2.35
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.636
Storage condition	2-8℃