GNE-375 ( GNE375 )

Catalog No. M13018 CAS No. 1926989-06-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-375
Note

Research use only, not for human use.
Brief Description

GNE-375 is a potent, selective BRD9 inhibitor with IC50 of 5 nM.
Description

GNE-375 is a potent, selective BRD9 inhibitor with IC50 of 5 nM, displays >480-fold selectivity over BRD4, CECR2, and TAF1; decreases BRD9 binding to chromatin, and decreases expression of ALDH1A1, a gene previously shown to be important in drug tolerance; shows remarkable potency in preventing the emergence of a drug tolerant population in EGFR mutant PC9 cells treated with EGFR inhibitors.
Synonyms

GNE375
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1926989-06-1
Formula Weight

451.52
Molecular Formula

C25H29N3O5
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C1C(NC=C2)=C2C(C3=CC(OC)=C(C(N4CCOCC4)=O)C=C3OC)=CN1C/C=C/C
Chemical Name

(E)-6-(but-2-en-1-yl)-4-(2,5-dimethoxy-4-(morpholine-4-carbonyl)phenyl)-2-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one

1. Crawford TD, et al. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3534-3541.

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