化学性质:
规格 | 10mg 50mg |
CAS | 901245-65-6 |
别名 |
|
化学名 | N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide |
分子式 | C22H26N4O3 |
分子量 | 394.47 |
溶解度 | ≥ 39.4mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
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.
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