Description
| Description | dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines. |
| Targets&IC50 | BRD9:56.6 nM |
| In vitro | DBRD9 (0.5-5000 nM; 4 h) reduces the expression of BRD9 in MOLM-13 cells in a concentration dependent manner with no significant effect on the expression of actin, BRD4, and BRD7. DBRD9 (100 nM; 2 hours) exhibits selectivity towards BRD9 in MOLM-13 cells. DBRD9 (7 days) exhibits anti-proliferative effects on EOL-1 and MOML-13 cell lines [1]. |
| Synonyms | dBRD9 HCl(2170679-45-3 Free base) |
| Molecular Weight |
856.75 |
| Formula | C40H47Cl2N7O10 |
| CAS No. | 2341840-98-8 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: 15.4 mg/mL (18.0 mM)
DMSO: 38.5 mg/mL (45.0 mM)
