MS023

MS023 is a potent, selective, and cell-active small molecule inhibitor of Type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4 (CARM1), and PRMT6. Developed as a chemical probe by the Structural Genomics Consortium (SGC), it specifically blocks the asymmetric dimethylation of arginine (ADMA) residues on various protein substrates, particularly RNA-binding proteins involved in splicing regulation. MS023 has been shown to preferentially kill leukemia cells harboring mutations in RNA splicing factors (such as SRSF2, SF3B1, and U2AF1) by reducing splicing fidelity and inducing apoptosis. It exhibits strong synergistic effects when used in combination with PRMT5 inhibitors or direct spliceosome inhibitors like E7107, highlighting its potential as a therapeutic agent for spliceosomal-mutant myeloid malignancies.

Other names

pan type I PRMT inhibitor