GNE-207

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1) . GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].

Product Specifications

CAS Number

[2158266-58-9]

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-207.html

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC)C1=NC=C(C2=CC3=C(C=N2)C(C4=NN(C5CCOCC5)C6=C4CN(C(C)=O)CC6)=CC=C3)C=C1

Molecular Formula

C29H30N6O3

Molecular Weight

510.59

References & Citations

[1]Lai KW, et al. Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300. ioorg Med Chem Lett. 2018 Jan 1;28 (1) :15-23.