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. . 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.

Product information

CAS Number: 1926986-36-8

Molecular Weight: 431.49

Formula: C24H25N5O3

Chemical Name: 6-(but-3-en-1-yl)-4-[1-methyl-6-(morpholine-4-carbonyl)-1H-1,3-benzodiazol-4-yl]-1H,6H,7H-pyrrolo[2,3-c]pyridin-7-one

Smiles: CN1C=NC2C(=CC(=CC1=2)C(=O)N1CCOCC1)C1=CN(CCC=C)C(=O)C2NC=CC1=2

InChiKey: XJRUWGFZGQNPPD-UHFFFAOYSA-N

InChi: InChI=1S/C24H25N5O3/c1-3-4-7-29-14-19(17-5-6-25-22(17)24(29)31)18-12-16(13-20-21(18)26-15-27(20)2)23(30)28-8-10-32-11-9-28/h3,5-6,12-15,25H,1,4,7-11H2,2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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