Home Epigenetics Epigenetic Reader Domain inhibitor GNE-781

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GNE-781 Epigenetic Reader Domain inhibitor

Cat.No.S8665

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. This compound also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. It exhibits antitumor activity.
GNE-781 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 525.59

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Quality Control

Batch: S866501 DMSO]125 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

Chemical Information, Storage & Stability

Molecular Weight 525.59 Formula

C27H33F2N7O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1936422-33-1 -- Storage of Stock Solutions

Synonyms N/A Smiles CNC(=O)N1CCC2=C(C1)C(=N[N]2C3CCOCC3)N4CCCC5=C4C=C(C(F)F)C(=C5)C6=C[N](C)N=C6

Solubility

In vitro
Batch:

DMSO : 125 mg/mL (237.82 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
CBP [1]
(in TR-FRET assay)
0.94 nM
BRET [1]
(Cell-free assay)
6.2 nM
BRD4(1) [1]
(Cell-free assay)
5100 nM
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. This compound decreases the generation of iTregs in vitro without affecting cell viability.[1]
In vivo

GNE-781, a highly potent and selective CBP inhibitor that is efficacious in a MOLM-16 AML xenograft model. In vivo, this compound modulates MYC expression that corresponds with antitumor activity in an AML tumor model.[1]
References

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