M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays.
M-525 inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively.
M-525 significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations.
M-525 also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.
