M-525 

M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC₅₀ of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity^[1].

M-525 achieves an IC₅₀ of 3 nM in the MV4;11 cell line and has an IC₅₀ of 2 µM in the HL-60 cell line. M-525 (3-300 nM; 24 h) is potent and effective in suppressing the expression of MEIS1 and HOX genes in MV4;11 cells carrying the MLL-AF4 fusion and in MOLM-13 cells carrying the MLL-AF9 fusion. It demonstrates high cellular specificity over non-MLL leukemia cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

734.92

C₃₉H₅₁FN₆O₅S

2173582-08-4

O=C(OC)N[C@@H]1[C@@H]([C@](C2CCN(CC3CN(C4=CC=C(S(=O)(C5CN(C(/C=C/CN(C)C)=O)C5)=O)C=C4)C3)CC2)(C#N)C6=CC=CC(F)=C6)CCC1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Xu S, et al. Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1601-1605.  [Content Brief]