Name: MS023
Price: 242.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 30, 119, 83, 4, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
    MS023 is a type I PRMTs inhibitor.
    Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. PRMT overexpression has been observed in a variety of human diseases including cancer. PRMTs has been divided into three categories: type I PRMTs for catalyzing mono- and asymmetric dimethylation of arginine residues, type II PRMTs for catalyzing mono- and symmetric dimethylation of arginine residues, and type III PRMT for catalyzing only monomethylation of arginine residues.
    In vitro: Previous study showed that MS023 had excellent potency for type I PRMTs but was completely inactive to both type II and type III PRMTs, protein lysine methyltransferases as well as DNA methyltransferases. Moreover, the crystal structure of PRMT6 with MS023 indicated that MS023 bound to the substrate binding site. In addition, MS023 could potently decrease the cellular levels of histone arginine asymmetric dimethylation. Furthermore, MS023 could reduce the levels of arginine asymmetric dimethylation and could also concurrently increase the cellular levels of both arginine monomethylation and symmetric dimethylation [1].
    In vivo: So far, there is no animal in vivo data reported.
    Clinical trial: Up to now, MS023 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine
    
    CAS Number
    
    1831110-54-3
    
    Molecular Formula
    
    C17H25N3O
    
    Molecular Weight
    
    287.4
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥28.7 mg/mL in DMSO; ≥13.7 mg/mL in EtOH; ≥23.3 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Wei Yuan, Qais Al-Hadid, et al. "TDRD3 promotes DHX9 chromatin recruitment and R-loop resolution." Nucleic Acids Res. 2021 Sep 7;49(15):8573-8591. PMID:34329467
    2. Pyun JH, Kim HJ, et al. "Cardiac specific PRMT1 ablation causes heart failure through CaMKII dysregulation." Nat Commun. 2018 Nov 30;9(1):5107. PMID:30504773

MS023

MS023

Background

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