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GNE-371

Catalog No.GC30529

GNE-371 est une sonde chimique puissante et sélective pour les deuxièmes bromodomaines de la sous-unité 1 TFIID du facteur d'initiation de la transcription humaine et de la sous-unité 1 du facteur d'initiation de la transcription TFIID, avec une IC50 de 10 nM pour TAF1(2).

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GNE-371 Chemical Structure

Cas No.: 1926986-36-8

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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.

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