AS-99 free base is a potent and selective inhibitor of the ASH1L histone methyltransferase, with an IC50 of 0.79 µM and a dissociation constant (Kd) of 0.89 µM. It demonstrates significant anti-leukemic activity by inhibiting cell proliferation, inducing apoptosis and differentiation, and downregulating MLL fusion target genes. AS-99 effectively reduces leukemia burden in vivo, making it a valuable tool for research into targeted therapies for leukemia and other ASH1L-related malignancies.
AS-99 free base is a potent and selective inhibitor of the ASH1L histone methyltransferase, with an IC50 of 0.79 µM and a dissociation constant (Kd) of 0.89 µM. It demonstrates significant anti-leukemic activity by inhibiting cell proliferation, inducing apoptosis and differentiation, and downregulating MLL fusion target genes. AS-99 effectively reduces leukemia burden in vivo, making it a valuable tool for research into targeted therapies for leukemia and other ASH1L-related malignancies.
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