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MS 4322

Cat. No. 8080 Submit a Review Datasheet / COA / SDS
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Description: Selective PRMT5 Degrader (PROTAC®)
Chemical Name: N-((S)-3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-((1-((S)-19-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidine-1-carbonyl)-20,20-dimethyl-17-oxo-3,6,9,12,15-pentaoxa-18-azahenicosanoyl)azetidin-3-yl)amino)pyrimidine-4-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 4322

MS 4322 is a protein arginine methyltransferase 5 (PRMT5) Degrader (PROTAC®) (DC50 = 1.1 μM, Dmax = 74% in MCF-7 cells). Inhibits PRMT5 methyltransferase activity (IC50 = 18 nM) and dose-dependently inhibits proliferation of HeLa, A549, A172 and Jurkat cancer cell lines. Comprises a PRMT5 inhibitor linked to an E3 ligase ligand.

Technical Data for MS 4322

M. Wt 1101.33
Formula C55H76N10O12S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2375432-47-4
PubChem ID 162652211
InChI Key XUJMNOQMXWVXQE-STHBVIMFSA-N
Smiles O=C(N1CC(C1)NC2=NC=NC(C(NC[C@H](O)CN3CC4=CC=CC=C4CC3)=O)=C2)COCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)=O)=O

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.

Solubility Data for MS 4322

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 110.13 100

Preparing Stock Solutions for MS 4322

The following data is based on the product molecular weight 1101.33. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.91 mL 4.54 mL 9.08 mL
5 mM 0.18 mL 0.91 mL 1.82 mL
10 mM 0.09 mL 0.45 mL 0.91 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

Molarity Calculator

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References for MS 4322

References are publications that support the biological activity of the product.

Shen et al (2020) Discovery of first-in-class protein arginine methyltransferase 5 (PRMT5) degraders. J.Med.Chem. 63 9977 PMID: 32787082

If you know of a relevant reference for MS 4322, please let us know.

View Related Products by Target

Keywords: MS 4322, MS 4322 supplier, MS4322, PRMT5, degraders, degrader, degrades, protein, arginine, methyltransferase, 5, PROTAC, proteolysis, targeting, chimera, VHL, E3, ligase, von, hippel, lindau, Other, Degraders, Protein, Arginine, Methyltransferases, 8080, Tocris Bioscience

Citations for MS 4322

Citations are publications that use Tocris products.

Currently there are no citations for MS 4322. Do you know of a great paper that uses MS 4322 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia