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GSK046 (iBET-BD2) is an effective, selective and orally active inhibitor of the BD2 bromine domain of the BET protein,IC50 The values are 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2), and 214 nM (BRDT BD2). GSK046 has immunomodulatory activity.
| Molecular Weight | 414.47 |
| Formula | C23H27FN2O4 |
| CAS Number | 2474876-09-8 |
| 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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