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MS023
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MS023图片
CAS NO:1831110-54-3
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 287.4
Formula C17H25N3O
CAS No. 1831110-54-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 30 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) CC(C)OC1=CC=C(C2=CNC=C2CN(C)CCN)C=C1
Synonyms MS023; MS-023; MS 023
实验参考方法
In Vitro

In vitro activity: MS023 is a novel potent, selective, and cell-active inhibitor of human type I PRMTs (Protein arginine methyltransferases) with IC50 ranging from 4 to 119 nM. PRMTs play a crucial role in a variety of biological processes. Overexpression of PRMTs has been implicated in various human diseases including cancer. MS023 displayed high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. A crystal structure of PRMT6 in complex with MS023 revealed that MS023 binds the substrate binding site. MS023 potently decreased cellular levels of histone arginine asymmetric dimethylation. It also reduced global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells. We also developed MS094, a close analog of MS023, which was inactive in biochemical and cellular assays, as a negative control for chemical biology studies.


Kinase Assay: MS023 displayed high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but was completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently inhibits PRMT1 (IC50 = 30 ± 9 nM), PRMT3 (IC50 = 119 ± 14 nM), PRMT4 (IC50 = 83 ± 10 nM), PRMT6 (IC50 = 4 ± 0.5 nM), and PRMT8 (IC50 = 5 ± 0.1 nM). Importantly, MS023 does not inhibit any type II PRMTs (PRMT5 and 9) and type III PRMT (PRMT7) at concentrations up to 10 μM. MS023 displays high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases.


Cell Assay: MS023 potently decreases cellular levels of histone arginine asymmetric dimethylation. It also reduces global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells.

In Vivo
Animal model
Formulation & Dosage
References ACS Chem Biol. 2016 Mar 18;11(3):772-781.