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。
货号:ajcx12402
CAS:1926986-36-8
分子式:C24H25N5O3
分子量：431.49
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.