MS023 (hydrochloride)
目录号 : GC16432An inhibitor of type I PRMTs
Cas No.:2108631-19-0
Sample solution is provided at 25 µL, 10mM.
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).
Cas No. | 2108631-19-0 | SDF | |
化学名 | 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 | ||
分子式 | C17H25N3O • 3HCl | 分子量 | 396.8 |
溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5202 mL | 12.6008 mL | 25.2016 mL |
5 mM | 0.504 mL | 2.5202 mL | 5.0403 mL |
10 mM | 0.252 mL | 1.2601 mL | 2.5202 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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