MS023, PRMT Inhibitor


Catalog No. size PriceQuantity
M60314-2S 2 mg solid $109
M60314-10S 10mg solid $452

Description

MS023 is a potent, selective and cell permeable type I PRMT inhibitor (catalyzes mono- and asymmetric dimethylation of arginine residues) with IC50 of 30 nM, 119 nM, 83 nM, 4 nM and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively. It is 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 reduces cellular levels of H4R3me2a in MCF7 and HEK293 cells by inhibiting PRMT1/6 methyltransferase activity with IC50 of 9 nM and 56 nM, respectively. It 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.

Product information

CAS Number: 1831110-54-3

Molecular Weight: 287.40

Formula: C17H25N3O

Chemical Name: N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine

Smiles: CC(C)OC1C=CC(=CC=1)C1=CNC=C1CN(C)CCN

InChiKey: FMTVWAGUJRUAKE-UHFFFAOYSA-N

InChi: InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM; EtOH up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

MS023 was used at 10 µM final concentration in various assays.

References:

  1. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. (2016) ACS Chem Biol. 11(3):772-81.

Products are for research use only. Not for human use.

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