Compound class:
Synthetic organic
Comment: MI-503 inhibits the interaction between MLL oncoproteins (re-arranged lysine methyltransferase 2A; KMT2A; a.k.a. MLL1) and the tumour suppressor protein menin (MEN1, O00255), by binding directly to MLL binding site on menin [1]. MI-503 is active in vivo, exhibiting selective antiproliferative effects on cells harbouring MLL rearrangements. It represents a highly optimised molecular scaffold for clinical lead identification in the development of drugs for the treatment of aggressive MLL-rearranged leukemias.
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Bioactivity Comments |
MI-503 binds to menin with a KD of 9.3nM, and inhibits the MLL-menin interaction with an IC50 of 14.7nM [1]. |