2158266-58-9

2158266-58-9 structure

Name: GNE-207
Chemical Name: GNE-207
CAS Number: 2158266-58-9
Molecular Formula: C₂₉H₃₀N₆O₃
Molecular Weight: 510.59
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2019-02-11 16:01:29
Modify Date: 2024-01-14 19:08:53
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].

Name	GNE-207

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	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Signaling Pathways >> Epigenetics >> Histone Acetyltransferase Research Areas >> Cancer
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.

Molecular Formula	C₂₉H₃₀N₆O₃
Molecular Weight	510.59