1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase

GNE-207 

Cat. No.: HY-120028
Handling Instructions

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.

For research use only. We do not sell to patients.

GNE-207 Chemical Structure

GNE-207 Chemical Structure

CAS No. : 2158266-58-9

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Description

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].

IC50 & Target[1]

CBP

1 nM (IC50)

BRD4(1)

3.1 μM (IC50)

In Vitro

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1].
GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].

In Vivo

GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1].

References
Molecular Weight

510.59

Formula

C₂₉H₃₀N₆O₃

CAS No.

2158266-58-9

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GNE-207
Cat. No.:
HY-120028
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GNE-207

Cat. No.: HY-120028