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GNE-272

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].

Product Specifications

CAS Number

[1936428-93-1]

UNSPSC

12352005

Target

Epigenetic Reader Domain; Histone Acetyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GNE-272.html

Purity

99.60

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[C@@H]5COCC5)C1)=O

Molecular Formula

C22H25FN6O2

Molecular Weight

424.47

References & Citations

[1]Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59 (23) :10549-10563.

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

CBP/p300

Available Sizes

Curated Selection

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