DDO-2093, a powerful inhibitor of the MLL1-WDR5 protein-protein interaction (IC50 = 8.6 nM; Kd = 11.6 nM), exhibits prominent antitumor effects. Notably, DDO-2093 selectively hampers the catalytic activity of the MLL complex.

DDO-2093 (5 μM; pretreated 7 days) inhibits MLL-fusion protein dependent genes expression ( HOXA9 and Meis1 )[1]. Western Blot Analysis[1]Cell Line: MV4-11 cells Concentration: 1, 2.5, 5, and 10 μM Incubation Time: Pretreated 7 days Result: Dose-dependently reduced the mono-, di-, and trimethylation of H3K4.

DDO-2093 (20 mg/kg-80 mg/kg; i.p.; every other day for 21 days) significantly suppresses the tumor size and weight in a dose-dependent manner[1]. Animal Model: Female nude mice (MV4-11 human leukemia cancer xenografts)[1]Dosage: 20 mg/kg, 40 mg/kg and 80 mg/kg Administration: I.p.; every other day for 21 days Result: The tumor volume growth inhibition (GI) values were calculated to be 13.7%, 37.6% and 63.9% with doses of 20 mg/kg, 40 mg/kg and 80 mg/kg, respectively.