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GNE-781

$170$2,780

Products Details

Product Description

– 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].

Web ID

– HY-108696

Storage Temperature

– -20°C (Powder, stored under nitrogen)

Shipping

– Blue Ice

Applications

– Cancer-programmed cell death

Molecular Formula

– C27H33F2N7O2

References

– [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.

CAS Number

– 1936422-33-1

Molecular Weight

– 525.59

Compound Purity

– 98.21

SMILES

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 100 mg/mL (ultrasonic)

Target

– Epigenetic Reader Domain;Histone Acetyltransferase

Isoform

– CBP/p300

Pathway

– Epigenetics

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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