AS-99 is a first-in-class, potent, and selective inhibitor of the ASH1L histone methyltransferase, displaying anti-leukemic activity with an IC50 of 0.79 µM and a Kd of 0.89 µM. It inhibits cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and effectively reduces leukemia burden [in vivo].
Molecular Weight:
630.14
Formula:
C27H31ClF3N5O3S2
Target:
Others|||Apoptosis|||Histone Methyltransferase
T73529
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