MS023 dihydrochloride 是一种有效选择性的，具有细胞活性的人I 型蛋白精氨酸甲基转移酶 (PRMTs)抑制剂，对PRMT1，PRMT3，PRMT4，PRMT6和PRMT8的IC50分别为 30，119，83，4 和 5 nM。

MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC 50 s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively [1].

MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells [1]. MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells [1]. Western Blot Analysis [1] Cell Line: MCF7 and HEK293 cells Concentration: 1.4, 4, 12, 37, 111, 333, and 1000 nM Incubation Time: 48 hours for MCF7 cells; 20 hours for HEK293 cells Result: Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC 50 =9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC 50 =56±7 nM).

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 [2]. Animal Model: NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells [2] 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.

1992047-64-9

C17H27Cl2N3O

360.32

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years