For research use only. Not for therapeutic Use.
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].
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].
GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1].
| Catalog Number | I019570 |
| CAS Number | 2158266-58-9 |
| Synonyms | 5-[8-[5-acetyl-1-(oxan-4-yl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]isoquinolin-3-yl]-N-methylpyridine-2-carboxamide |
| Molecular Formula | C29H30N6O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H30N6O3/c1-18(36)34-11-8-27-24(17-34)28(33-35(27)21-9-12-38-13-10-21)22-5-3-4-19-14-26(32-16-23(19)22)20-6-7-25(31-15-20)29(37)30-2/h3-7,14-16,21H,8-13,17H2,1-2H3,(H,30,37) |
| InChIKey | MUJXZEDIWKGKQD-UHFFFAOYSA-N |
| SMILES | CC(=O)N1CCC2=C(C1)C(=NN2C3CCOCC3)C4=CC=CC5=CC(=NC=C54)C6=CN=C(C=C6)C(=O)NC |
| Reference | [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. |
