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GNE-371

Chemical Structure : GNE-371

CAS No.: 1926986-36-8

GNE-371 (GNE371;GNE 371)

Catalog No.: PC-35709Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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).
GNE-371 exhibits antiproliferative synergy with the BET inhibitor JQ1, suggesting engagement of endogenous TAF1 by GNE-371.

Physicochemical Properties

M.Wt 431.496
Formula C24H25N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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