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 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).

2408842-51-1

C30H31FN4O3

514.59

WDR5-IN-1

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years