MI-1481

MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503; markedly reduces cell growth of murine bone marrow cells transformed with MLL-AF9 with GI50 of 34 nM, demonstrates potent on target activity in MLL leukemia cells with GI50 values of 36 nM in MV4;11 (harboring MLL-AF4 fusion protein) and 61 nM in MOLM13 (harboring MLL-AF9); downregulates the MLL fusion protein target genes, HOXA9 and MEIS1, at 100 nMin MV4;11 human MLL leukemia cells; strongly inhibits leukemia progression in vivo.

References 1. Borkin D, et al. J Med Chem. 2018 May 23. doi: 10.1021/acs.jmedchem.8b00071. View Related Products by Target Histone Methyltransferase (HMTase)