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GSK 5959
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK 5959图片
CAS NO:901245-65-6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
GSK 5959 是一种有效的、选择性的和细胞可渗透的 BRPF1 溴结构域抑制剂,IC50 为 ~ 80 nM。
Cas No.901245-65-6
化学名N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide
Canonical SMILESO=C(C1=C(C=CC=C1)OC)NC2=C(C=C(N(C)C(N3C)=O)C3=C2)N4CCCCC4
分子式C22H26N4O3
分子量394.47
溶解度≥ 39.4mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.

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.