AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 µM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 µM[1].
AS-85 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations, with GI50 values ranging from 5 µM to 25 µM, and demonstrates no effect in K562 leukemia cells without MLL1 translocations[1].