For research use only. Not for therapeutic Use.
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM[1].
MS117 (Compound 4) inhibits the PRMT6 methyltransferase activity in a time-dependent manner[1].
MS117 (Compound 4) shows moderate selectivity (6-fold) for PRMT6 over PRMT1 (IC50 = 0.1 ± 0.025 µM) and PRMT8 (IC50 = 0.11 ± 0.01 µM) [1].
| Catalog Number | I045829 |
| CAS Number | 2702280-86-0 |
| Synonyms | N-[3-[4-[[2-aminoethyl(methyl)amino]methyl]-1H-pyrrol-3-yl]phenyl]prop-2-enamide |
| Molecular Formula | C17H22N4O |
| Purity | ≥95% |
| InChI | InChI=1S/C17H22N4O/c1-3-17(22)20-15-6-4-5-13(9-15)16-11-19-10-14(16)12-21(2)8-7-18/h3-6,9-11,19H,1,7-8,12,18H2,2H3,(H,20,22) |
| InChIKey | HVDMIAFOVVMNJF-UHFFFAOYSA-N |
| SMILES | CN(CCN)CC1=CNC=C1C2=CC(=CC=C2)NC(=O)C=C |
| Reference | [1]. Yudao Shen, et al. Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. J Med Chem. 2020 May 28;63(10):5477-5487. |
