2. Immunology/Inflammation
  3. Fc Receptor (FcR)
  4. 2158266-58-9

2158266-58-9

GNE-207 Chemical Structure

2158266-58-9

Chemical Structure

  • GNE-207
  • CAS No: 2158266-58-9
    Formula: C29H30N6O3
    Molecular Weight: 510.59
  • IUPAC Name: 5-(8-(5-acetyl-1-(tetrahydro-2H-pyran-4-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)isoquinolin-3-yl)-N-methylpicolinamide
  • InChIKey: MUJXZEDIWKGKQD-UHFFFAOYSA-N
  • 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

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

Cat. No. Product Name Purity Description
HY-120028 GNE-207 99.94% GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.

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. [Content Brief]

Keywords:

GNE-207