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MS 147

Cat. No. 8077 Submit a Review Datasheet / COA / SDS
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Description: PRC1 Degrader (PROTAC®); degrades BMI1 and RING1B
Chemical Name: (2S,4R)-1-((S)-2-(7-(5-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)phenyl)piperazin-1-yl)pentanamido)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 147

MS 147 is a polycomb repressive complex 1 (PRC1) Degrader (PROTAC®) (Kd values are 450 nM and 3 μM for VHL and EED, respectively). Comprises an EED binder (EED 226, Cat. No. 7762) joined by a linker to a VHL E3 ligase ligand. MS 147 preferentially degrades BMI1 and RING1B and reduces H2AK119ub in K562 cells. Inhibits proliferation in cancer cell lines that are insensitive to EZH2 knockout or EED/PRC2 Degraders.

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

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Important Information for MS 147

This product is sold as an HCl salt. The stoichiometry of the salt and hydration levels vary from batch to batch. It is sold in gross weight and the batch specific Molecular Weight is available on the Certificate of Analysis.

Technical Data for MS 147

M. Wt 1015.29 (Free Base)
Formula C54H70N12O6S.xHCl
Storage Store at -20°C
Purity ≥97% (HPLC)
InChI Key WZUKNVLQEQHTMY-RTJWYONCSA-N
Smiles CC1=C(C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCCCCNC(CCCCN4CCN(C5=CC=C(C6=CN=C(NCC7=CC=CO7)N8C6=NN=C8)C=C5)CC4)=O)=O)C(C)(C)C)=O)=O)C=C2)SC=N1.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.

Solubility Data for MS 147

Solubility Soluble to 50 mg/ml in DMSO

References for MS 147

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

Park et al (2023) Targeted degradation of PRC1 components, BMI1 and RING1B, via a novel protein complex degrader strategy. Adv.Sci. (Weinh.) 10 e2205573 PMID: 36737841

If you know of a relevant reference for MS 147, please let us know.

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Citations for MS 147

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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