CAS NO: | 1831110-54-3 |
包装 | 价格(元) |
5mg | 询价 |
25mg | 询价 |
Cas No. | 1831110-54-3 |
别名 | N1-甲基-N1-[[4-[4-(异丙氧基)苯基]-1H-吡咯-3-基]甲基]-1,2-乙二胺 |
化学名 | N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine |
Canonical SMILES | NCCN(C)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2 |
分子式 | C17H25N3O |
分子量 | 287.4 |
溶解度 | ≥ 28.7mg/mL in DMSO |
储存条件 | Store at -20℃ |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IC50: 30, 119, 83, 4, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. MS023 is a type I PRMTs inhibitor. Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. PRMT overexpression has been observed in a variety of human diseases including cancer. PRMTs has been divided into three categories: type I PRMTs for catalyzing mono- and asymmetric dimethylation of arginine residues, type II PRMTs for catalyzing mono- and symmetric dimethylation of arginine residues, and type III PRMT for catalyzing only monomethylation of arginine residues. In vitro: Previous study showed that MS023 had excellent potency for type I PRMTs but was completely inactive to both type II and type III PRMTs, protein lysine methyltransferases as well as DNA methyltransferases. Moreover, the crystal structure of PRMT6 with MS023 indicated that MS023 bound to the substrate binding site. In addition, MS023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. Furthermore, MS023 could reduce the levels of arginine asymmetric dimethylation and could also concurrently increase the cellular levels of both arginine monomethylation and symmetric dimethylation [1]. In vivo: So far, there is no animal in vivo data reported. Clinical trial: Up to now, MS023 is still in the preclinical development stage. Reference: |
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