GNE-371

Modify Date: 2024-01-10 11:06:18

GNE-371 Structure
GNE-371 structure
Common Name GNE-371
CAS Number 1926986-36-8 Molecular Weight 431.49
Density N/A Boiling Point N/A
Molecular Formula C24H25N5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GNE-371


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).

 Names

Name GNE-371

 GNE-371 Biological Activity

Description 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).
Related Catalog
Target

IC50: 10 nM (TAF1(2))[1].

In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C24H25N5O3
Molecular Weight 431.49
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