GNE-049 ( GNE049;GNE 049 )

Catalog No. M13034 CAS No. 1936421-41-8

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GNE-049
Note

Research use only, not for human use.
Brief Description

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
Description

GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively; displays 3,850-fold selectivity over BRD4; shows excellent potency (12 nM) in a BRET cellular assay and inhibits the expression of MYC with EC50 of 14 nM in MV-4-11 cells; demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo.
Synonyms

GNE049;GNE 049
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

——
Indication

——

CAS Number

1936421-41-8
Formula Weight

510.59
Molecular Formula

C27H32F2N6O2
Purity

>98% (HPLC)
Solubility

DMSO : 100 mg/mL 195.86 mM
SMILES

CC(N1CCC(N(C2COCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O
Chemical Name

1-(3-(7-(difluoromethyl)-6-(1-methyl-1H-pyrazol-4-yl)-3,4-dihydroquinolin-1(2H)-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one

1. Jin L, et al. Cancer Res. 2017 Aug 17. pii: canres.0314.2017.

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