| Description | BI-9321 is a selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist (Kd: 166 nM). BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. |
| In vitro | BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain (IC50: 1.2 μM in U2OS cells). BI-9321 is targeting the methyl-lysine binding site of the PWWP1 domain and cellular target engagement at 1?μM. BI-9321 downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells. |
| Target activity | NSD3-PWWP1:(kd)166 nM |
| molecular weight | 360.43 |
| Molecular formula | C22H21FN4 |
| CAS | 2387510-86-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829. |