Home Epigenetics Epigenetic Reader Domain inhibitor GNE-781 For research use only.

GNE-781

GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.

GNE-781 Chemical Structure

GNE-781 Chemical Structure

CAS No. 1936422-33-1

Purity & Quality Control

Batch: S866501 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

GNE-781 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
Targets
CBP [1]
(in TR-FRET assay)		 BRET [1]
(Cell-free assay)		 BRD4(1) [1]
(Cell-free assay)
0.94 nM 6.2 nM 5100 nM
In vitro
In vitro

In vitro studies show that GNE-781 reduces FOXP3 (forkhead box P3) transcript levels with a less optimal chemical probe, suggesting that inhibition of the CBP bromodomain may provide a novel small molecule therapeutic approach for cancer immunotherapy. GNE-781 decreases the generation of iTregs in vitro without affecting cell viability.[1]
Cell Research Cell lines MV-4-11
Concentrations 0.002-12.7 μM
Incubation Time 4 h
Method

To determine the inhibition of MYC expression, MV-4-11 cells (ATCC) sre plated at 10000 cells per well in 96-well plates in RPMI1640 media supplemented with 10% fetal bovine serum and 2 mM L-glutamine. GNE-781 diluted in DMSO are transferred to the cell plates, keeping final DMSO concentration consistent at 0.1%, and incubated for 4 h at 37 °C. Lysis and analysis for MYC expression are carried out using QuantiGene 2.0 reagents and following the vendor’s instructions. Luminescence is read using an EnVision plate reader and EC50s are generated in XLFit using a fourparameter nonlinear regression fit.
In Vivo
In vivo

GNE-781, a highly potent and selective CBP inhibitor that is efficacious in a MOLM-16 AML xenograft model. In vivo, GNE-781 modulates MYC expression that corresponds with antitumor activity in an AML tumor model.[1]
Animal Research Animal Models female 6−9 week-old CD-1 mice
Dosages 3-30 mg/kg, 1 mg/kg
Administration Oral gavage, IV

Chemical Information & Solubility

Molecular Weight 525.59 Formula

C27H33F2N7O2
CAS No. 1936422-33-1 SDF --
Smiles CNC(=O)N1CCC2=C(C1)C(=N[N]2C3CCOCC3)N4CCCC5=C4C=C(C(F)F)C(=C5)C6=C[N](C)N=C6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (190.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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