ML399 

ML399 is a second-generation probe optimized for inhibitors of menin-mixed lineage leukemia (MLL) protein-protein interactions. Screening through the Molecular Library Probe Production Network (MLPCN) led to the discovery of several chemical classes, including piperidines, which successfully led to the generation of the first-generation probe ML227. However, metabolic instability, potency, and adjuvant pharmacological activity of ML227 were identified as limiting features. To enhance the utility of menin-MLL inhibitor probes for in vivo mechanistic studies, medicinal chemistry efforts were reinvigorated using a structure-based design approach, which ultimately led to the generation of the announced probe ML399. This study describes the structure-activity relationships and properties of this series of compounds.

445.53

C₂₇H₂₈FN₃O₂

1560968-49-1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Progress towards small molecule inhibitors of the Menin-Mixed Lineage Leukemia (MLL) interaction with in vivo utility