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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD4; CBP/p300
Available Sizes
Frequently Asked Questions
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