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2158266-58-9

2158266-58-9 structure
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: 2025-08-27 09:38:56
  • 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
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
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