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MS023 (hydrochloride)

Catalog No.
C3503
type I PRMTs inhibitor
Grouped product items
SizePriceStock Qty
1mg
$85.00
Ship with 10-15 days
5mg
$350.00
Ship with 10-15 days
10mg
$615.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt396.8
Cas No.2108631-19-0
FormulaC17H25N3O·3HCl
Solubility≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical NameN1-​methyl-​N1-​[[4-​[4-​(1-​methylethoxy)​phenyl]​-​1H-​pyrrol-​3-​yl]​methyl]​-1,​2-​ethanediamine, trihydrochloride
SDFDownload SDF
Canonical SMILESCC(C)OC1=CC=C(C2=CNC=C2CN(C)CCN)C=C1.Cl.Cl.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

MS023 (hydrochloride)