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Submit ReviewCM 11 is a 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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under licence from the University of Dundee
E3 ligase | VHL |
DC50 | 10-100 nM - Degradation of pVHL30 in HeLa cells after 24 h treatment |
Selectivity confirmed by global proteomics | No |
M. Wt | 1179.46 |
Formula | C58H82N8O14S2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 2244684-49-7 |
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 117.95 | 100 |
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 |
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, PROTAC, active, degraders, degrades, protein, degradation, tpd, Ubiquitin, Ligases, Ligase, Degraders, 6416, Tocris Bioscience
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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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