GNE-781 - 98%, high purity , CAS No.1936422-33-1

Item Number

G414103

• Specifications & Purity: ≥98%
• Biochemical and Physiological Mechanisms: 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 o
• Storage Temp: Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads

Product Description

Information

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.

Targets

CBP (in TR-FRET assay); BRET (Cell-free assay); BRD4(1) (Cell-free assay) 0.94 nM; 6.2 nM; 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. GNE-781 decreases the generation of iTregs in vitro without affecting cell viability.

In vivo

GNE-781, a highly potent and selective CBP inhibitor that is efficacious in a MOLM-16 AML xenograft model. GNE-781 modulates MYC expression that corresponds with antitumor activity in an AML tumor model.

Cell Research(from reference)

Cell lines：MV-4-11 

Concentrations：0.002-12.7 μM 

Incubation Time：4 h