GNE-049

GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4 (1) with IC50s of 12 nM and 4200 nM, respectively[1].

Product Specifications

CAS Number

[1936421-41-8]

UNSPSC

12352005

Hazard Statement

H315-H319-H335

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-049.html

Concentration

10mM

Purity

99.33

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C27H32F2N6O2

Molecular Weight

510.58

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501

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.