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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CBP/p300
Available Sizes
Curated Selection
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