MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
48 hours for MCF7 cells; 20 hours for HEK293 cells
Result:
Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC50=9±0.2 nM).
Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56±7 nM).
体内研究
Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells.
Animal Model:
NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells
Dosage:
160 mg/kg
Administration:
Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result:
Combinatorial treatment extended survival of leukemic mice relative to single treatments.
分子式
C17H25N3O
分子量
287.40
CAS号
1831110-54-3
运输条件
Room temperature in continental US; may vary elsewhere.