AS-99 free base

Description: AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity, blocking cell proliferation, inducing apoptosis and differentiation, downregulating MLL fusion target genes, and reducing the leukemia burden in vivo[1]. Target: Others. Smiles: CN1CC(C1)C(=O)NCc1ccc2c(cn(C3CCN(CC3)S(=O)(=O)C(F)(F)F)c2c1)-c1cccc(c1)C(N)=S. References: David S. Rogawski, Jing Deng, Hao Li, Tomasz Cierpicki, Jolanta Grembecka, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14,12(1):2792.