For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I019102 |
| CAS Number | 1992047-64-9 |
| Synonyms | N’-methyl-N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine;dihydrochloride |
| Molecular Formula | C17H27Cl2N3O |
| Purity | ≥95% |
| InChI | InChI=1S/C17H25N3O.2ClH/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18;;/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3;2*1H |
| InChIKey | HCNXCUFNZWGILO-UHFFFAOYSA-N |
| SMILES | CC(C)OC1=CC=C(C=C1)C2=CNC=C2CN(C)CCN.Cl.Cl |
| Reference | [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. [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. |
