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GNE-781 (compound 19) is a highly potent, orally active, selective bromodomain inhibitor against cyclic adenosine monophosphate response element binding protein (CBP). The IC50 value is 0.94 nM (in TR-FRET assay). GNE-781 also suppresses BRET and BRD4(1), with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 has antitumor activity.
| Molecular Weight | 525.59 |
| Formula | C27H33F2N7O2 |
| CAS Number | 1936422-33-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| dBRD9 dihydrochloride
dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. |
| BBC0403
BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. |
| BAY-155
BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. |
| FHT-1015
FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC50s of ≤10 nM. |
| ISOX-DUAL
ISOX-DUAL is a dual CBP/BRD4 inhibitor with IC50 values of 0.65 μM and 1.5 μM for CBP and BRD4, respectively. |
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