AS-99 free base

Description

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor IC50=?0.79?AAasAasAAmuM, Kd=?0.89?AAasAasAAmuM with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.