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Submit ReviewMS 023 dihydrochloride is a potent and selective type I PRMT inhibitor (IC50 values are 8, 8, 30, 83 and 119 nM for PRMT6, PRMT8, PRMT1, PRMT4 and PRMT3, respectively). Exhibits no significant activity against type II and III PRMTs, PKMTs, DNMTs, KDMs and reader proteins. Reduces global arginine asymmetric dimethylation levels in vitro. Also inhibits and reduces TGF-β-activated kinase 1 expression and protein levels.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the MS023 probe summary on the SGC website.
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MS023 is reviewed on the chemical probes website.
M. Wt | 360.32 |
Formula | C17H25N3O.2HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1992047-64-9 |
PubChem ID | 121513886 |
InChI Key | HCNXCUFNZWGILO-UHFFFAOYSA-N |
Smiles | CC(C)OC1=CC=C(C2=CNC=C2CN(CCN)C)C=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 36.03 | 100 | |
DMSO | 36.03 | 100 |
The following data is based on the product molecular weight 360.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.78 mL | 13.88 mL | 27.75 mL |
5 mM | 0.56 mL | 2.78 mL | 5.55 mL |
10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
Eram et al (2016) A potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases. ACS Chem.Biol. 11 772 PMID: 26598975
Scheer et al (2019) A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. Nat.Commun. 11 19 PMID: 30604761
If you know of a relevant reference for MS 023 dihydrochloride, please let us know.
Keywords: MS 023 dihydrochloride, MS 023 dihydrochloride supplier, MS023, dihydrochloride, potent, Type-1, selective, PRMT, inhibitors, inhibits, PRMT6, PRMT8, PRMT1, PRMT4, PRMT3, Protein, Arginine, Methyltransferases, 5713, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for MS 023 dihydrochloride include:
Tang et al (2022) A genome-scale CRISPR screen reveals PRMT1 as a critical regulator of androgen receptor signaling in prostate cancer. Cell Rep. 38 110417 PMID: 35196489
Lu et al (2021) Pharmacologic modulation of RNA splicing enhances anti-tumor immunity. Cell PMID: 34171309
Choucair et al (2019) The arginine methyltransferase PRMT1 regulates IGF-1 signaling in breast cancer. Oncogene 38 4015 PMID: 30692633
Do you know of a great paper that uses MS 023 dihydrochloride from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.