| CAS NO: | 2108631-19-0 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 396.8 |
| Cas No. | 2108631-19-0 |
| Formula | C17H25N3O·3HCl |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | N1-methyl-N1-[[4-[4-(1-methylethoxy)phenyl]-1H-pyrrol-3-yl]methyl]-1,2-ethanediamine, trihydrochloride |
| Canonical SMILES | CC(C)OC1=CC=C(C2=CNC=C2CN(C)CCN)C=C1.Cl.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively
MS023 is a type I PRMT inhibitor.
Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. Overexpression of PRMTs is implicated in various human diseases, such as cancer. Thus, selective inhibitors of PRMTs have been pursued by both academia as chemical tools for evaluating biological and therapeutic hypotheses.
In vitro: MS023 was identified to have high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was inactive against type II and type III PRMTs, protein lysine methyltransferases as well as DNA methyltransferases. The crystal structure of PRMT6 with MS023 indicated that MS023 bound to the substrate binding site. Moreover, MS023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. In cells, MS023 also ould reduce the levels of arginine asymmetric dimethylation and increase levels of arginine monomethylation and symmetric dimethylation. Therefore, MS023 is a useful chemical tool for testing the role of type I PRMTs in health and disease [1].
In vivo: So far, there is no animal data reported.
Clinical trial: Up to now, MS023 is still in the preclinical development stage.
Reference:
[1] M. S. Eram, Y. Shen, M. M. Szewczyk, et al. A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases. ACS Chemical Biology 11.8.15, (2015).
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