CM 11

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Cat.No. 6416 - CM 11 | C58H82N8O14S2
Description: Homo-PROTAC for self-degradation of pVHL30
Chemical Name: N1,N20-bis((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,6,9,12,15,18-hexaoxaicosanediamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Homo-PROTAC for self-degradation of the long form of VHL, pVHL30 (DC50 < 100 nM). Composed of two VHL ligands joined by a linker. Exhibits > 1000-fold increased cellular activity compared to the parent VHL ligand, VH 032. Dimerizes pVHL30 with high avidity in vitro. Induced potent and rapid self-degradation of VHL in cell lines in a highly isoform dependent fashion. Negative control CMP 98 (Cat. No. 6417) also available.

PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells.

Licensing Information

Sold under licence from the University of Dundee

Technical Data

M. Wt 1179.46
Formula C58H82N8O14S2
Storage Store at -20°C
Purity ≥98% (HPLC)
PubChem ID 134160242
InChI Key WGJCHHJGGFCCRS-DEYDLUNASA-N
Smiles CC1=C(C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=O)=O)=O)C=C2)SC=N1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 117.95 100
ethanol 117.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 1179.46. 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 0.85 mL 4.24 mL 8.48 mL
5 mM 0.17 mL 0.85 mL 1.7 mL
10 mM 0.08 mL 0.42 mL 0.85 mL
50 mM 0.02 mL 0.08 mL 0.17 mL

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References

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

Maniaci et al (2017) Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. Nat.Commun. 8 830 PMID: 29018234


If you know of a relevant reference for CM 11, please let us know.

Keywords: CM 11, CM 11 supplier, CM11, PROTACs, Proteolysis, targeted, chimeras, E3, ubiquitin, ligase, VHL, Ubiquitin, Ligases, Active, Degraders, 6416, Tocris Bioscience

Citations for CM 11

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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* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders (e.g. PROTACs)
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Epigenetics

Epigenetics Scientific Review

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.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation

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.