| Description | WDR5-IN-1 is a potent and selective inhibitor of WD repeat domain 5 (WDR5) (Kd <0.02 nM), and also inhibits MLL1 histone methyltransferase (HMT) activity (IC50: 2.2 nM). |
| In vitro | In G2M phase cells, WDR5-IN-1 (1 μM; 48 hours) shows an apparent decrease . WDR5-IN-1 (0.01-3 μM; 24-48 hours) increases p53 and p21 protein levels. WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells)(GI50s : 0.26-3.2 μM). |
| molecular weight | 514.59 |
| Molecular formula | C30H31FN4O3 |
| CAS | 2408842-51-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675. |