GNE-371( GNE371 | GNE 371 )

Catalog No. M13017 CAS No. 1926986-36-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-371
Note

Research use only, not for human use.
Brief Description

GNE-371 (GNE371) is a highly potent and selective chemical probe for the second bromodomain of TAF1 (TAF1(2)) with IC50/Kd of 10/1 nM.
Description

GNE-371 (GNE371) is a highly potent and selective chemical probe for the second bromodomain of TAF1 (TAF1(2)) with IC50/Kd of 10/1 nM, without significant activity against other bromodomain-family members; GNE-371 (GNE371) 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.
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.
In Vivo

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Synonyms

GNE371 | GNE 371
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

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CAS Number

1926986-36-8
Formula Weight

431.496
Molecular Formula

C24H25N5O3
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (115.88 mM)
SMILES

O=C1C(NC=C2)=C2C(C3=C4N=CN(C)C4=CC(C(N5CCOCC5)=O)=C3)=CN1CCC=C
Chemical Name

6-But-3-enyl-4-[1-methyl-6-(morpholine-4-carbonyl)-benzimidazol-4-yl]-1H-pyrrolo[2,3-c]pyridin-7-one

1. Wang S, et al. J Med Chem. 2018 Oct 25;61(20):9301-9315.

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