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MS023 dihydrochloride 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[1]. | [in vivo]
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. |
| [IC 50]
PRMT1; PRMT3; PRMT6; PRMT8 | [storage]
Store at -20°C | [References]
[1] Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81. DOI:10.1021/acschembio.5b00839
[2] Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268. DOI:10.1182/blood.2019002457 |
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InvivoChem
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https://www.invivochem.cn/ |
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