MedKoo Cat#: 206990 | Name: GNE-371
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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. GNE-371 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 antiproliferative 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.

Chemical Structure

GNE-371
GNE-371
CAS#1926986-36-8

Theoretical Analysis

MedKoo Cat#: 206990

Name: GNE-371

CAS#: 1926986-36-8

Chemical Formula: C24H25N5O3

Exact Mass: 431.1957

Molecular Weight: 431.50

Elemental Analysis: C, 66.81; H, 5.84; N, 16.23; O, 11.12

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
10mg USD 1,250.00 2 Weeks
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Related CAS #
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Synonym
GNE-371; GNE 371; GNE371
IUPAC/Chemical Name
6-But-3-enyl-4-[1-methyl-6-(morpholine-4-carbonyl)-benzimidazol-4-yl]-1H-pyrrolo[2,3-c]pyridin-7-one
InChi Key
XJRUWGFZGQNPPD-UHFFFAOYSA-N
InChi Code
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
SMILES Code
O=C1C(NC=C2)=C2C(C3=C4N=CN(C)C4=CC(C(N5CCOCC5)=O)=C3)=CN1CCC=C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
TAF1 contains both a histone acetyltransferase (HAT) domain and a tandem bromodomain module, comprising the individual bromodomains TAF1(1) and TAF1(2). Although the function of TAF1 has not been fully elucidated, it has been implicated in pathways associated with cancer.

Preparing Stock Solutions

The following data is based on the product molecular weight 431.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. 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 5. doi: 10.1021/acs.jmedchem.8b01225. [Epub ahead of print] PubMed PMID: 30289257.