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GNE-371
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。
GNE-371图片
CAS NO:1926986-36-8
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
GNE-371是一种针对人类转录起始因子TFIID亚基1和类转录起始因子TFIID亚基1的第二溴端结构域的高效选择性化学探针,对TAF1(2)的IC50值为10nM。
Cas No.1926986-36-8
Canonical SMILESO=C1C(NC=C2)=C2C(C3=C4N=CN(C)C4=CC(C(N5CCOCC5)=O)=C3)=CN1CCC=C
分子式C24H25N5O3
分子量431.49
溶解度Soluble in DMSO
储存条件Store at -20°C
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

GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).

GNE-371 (compound 27) binds TAF1(2) with an IC50 of 10 nM while maintaining excellent selectivity over other bromodomain-family members. GNE-371 is also active in a cellular-TAF1(2) target-engagement assay (IC50=38 nM) and exhibits anti-proliferative synergy with the BET inhibitor JQ1, suggesting engagement of endogenous TAF1 by GNE-371 and further supporting the use of GNE-371 in mechanistic and target-validation studies[1].

[1]. Wang S, et al. GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like. J Med Chem. 2018 Oct 25;61(20):9301-9315.