GNE-781

GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4 (1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model[1].

Product Specifications

CAS Number

[1936422-33-1]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Histone Acetyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GNE-781.html

Purity

98.16

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)NC

Molecular Formula

C27H33F2N7O2

Molecular Weight

525.59

References & Citations

[1]Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) . J Med Chem. 2017 Nov 22;60 (22) :9162-9183.