GNE-207

Modify Date: 2024-01-14 19:08:53

GNE-207 Structure
GNE-207 structure
Common Name GNE-207
CAS Number 2158266-58-9 Molecular Weight 510.59
Density N/A Boiling Point N/A
Molecular Formula C29H30N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GNE-207


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].

 Names

Name GNE-207

 GNE-207 Biological Activity

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].
Related Catalog
Target

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

[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.

 Chemical & Physical Properties

Molecular Formula C29H30N6O3
Molecular Weight 510.59
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