Description
| Description | HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively). |
| Targets&IC50 | BRD4 BD1:7.0nM, BRD4 BD1:0.5nM, Plusmn:0.7 nM, Plusmn:0.6 nM, Plusmn:0.5 nM, Plusmn:0.4 nM, Plusmn:0.2 nM (ki), Plusmn:0.2 nM, Plusmn:0.1 nM （ki）, Plusmn:0.09 nM (ki), Plusmn:0.03 nM （ki）, Plusmn:0.01 nM （ki）, BRD2 BD2:3.9nM, BRD2 BD2:0.27nM(ki), BRD3 BD2:1.9nM, BRD3 BD2:0.21nM, BRD2 BD1:3.1nM, BRD2 BD1:0.9(ki), BRD3 BD1:6.6nM, BRD3 BD1:0.18nM, BRD4 BD2:7.0nM, BRD4 BD2:1.0nM |
| In vitro | HJB97 is a highly potent and extra terminal (BET) inhibitor (IC50s of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), 7.0 nM (BRD4 BD1), 7.0 nM (BRD4 BD2)). HJB97 can potently down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cell line (treated for 24 h). HJB97 (10-1000 nM, 4 days) effectively inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines (IC50s: 24.1 nM and 25.6 nM)[1]. |
| Molecular Weight |
500.55 |
| Formula | C26H28N8O3 |
| CAS No. | 2093391-24-1 |
Storage
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 27.0 mg/mL (53.9 mM),
Sonication is recommended.
H2O: insoluble
