ML399

ML399 is a Menin-MLL1 protein-protein interaction inhibitor with an IC₅₀ of 90 nM. ML399 inhibits the proliferation of transformed mouse bone marrow cells. ML399 binds to the hERG potassium channel, exhibits superior in vitro physicochemical, drug metabolism and pharmacokinetic (DMPK) parameters, and has an extended half-life in rodents. ML399 can be used for research on acute myeloid leukemia and acute lymphoblastic leukemia^[1]. In Vitro:ML399 (72 h) inhibits proliferation of MLL-AF9-transformed murine bone marrow cells with a GI₅₀ of 4 μM^[1].
ML399 exhibits improved in vitro DMPK properties, with human microsomal intrinsic clearance of 20 mL/min/kg, predicted human hepatic clearance of 10 mL/min/kg, and plasma protein binding fraction unbound values of 0.062 (human), 0.074 (rat), and 0.079 (mouse)^[1].