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MS 159

Cat. No. 8079 Submit a Review Datasheet / COA / SDS
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Description: NSD2 Degrader (PROTAC®)
Chemical Name: N-Cyclopropyl-N-(4-((5-(3-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)propoxy)pyridin-2-yl)-carbamoyl)benzyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 159

MS 159 is a nuclear receptor binding SET structural domain protein 2 (NSD2) Degrader (DC50 = 5.2 μM, Dmax = >82%). Also degrades IKZF3 and IKZF1. Comprises an NSD2 binding moiety joined by a linker to a cereblon E3 ligase ligand. Inhibits proliferation of KMS11 and H929 tumor cells. Bioavailable in vivo.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for MS 159

M. Wt 828.84
Formula C43H40N8O10
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 3031353-59-7
PubChem ID 164887575
InChI Key OBZWKPGPTCBYOS-UHFFFAOYSA-N
Smiles O=C(NC1=NC=C(OCCCNC(CNC2=CC=CC3=C2C(N(C4CCC(NC4=O)=O)C3=O)=O)=O)C=C1)C(C=C5)=CC=C5CN(C(C6=CC7=C(NC(CO7)=O)C=C6)=O)C8CC8

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 159

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.44 50

Preparing Stock Solutions for MS 159

The following data is based on the product molecular weight 828.84. 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
0.5 mM 2.41 mL 12.07 mL 24.13 mL
2.5 mM 0.48 mL 2.41 mL 4.83 mL
5 mM 0.24 mL 1.21 mL 2.41 mL
25 mM 0.05 mL 0.24 mL 0.48 mL

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References for MS 159

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

Meng et al (2022) Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos. J.Med.Chem. 65 10611 PMID: 35895319

If you know of a relevant reference for MS 159, please let us know.

View Related Products by Target

Keywords: MS 159, MS 159 supplier, MS159, degrader, degrades, degradation, NSD2, nuclear, receptor, binding, SET, structural, domain, protein, 2, PROTAC, proteolysis, targeting, chimeras, CRBN, cereblon, E3, ligase, WHSC1, MMSET, Other, Degraders, 8079, Tocris Bioscience

Citations for MS 159

Citations are publications that use Tocris products.

Currently there are no citations for MS 159. Do you know of a great paper that uses MS 159 from Tocris? Please let us know.

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Literature in this Area

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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