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Biological Activity for TCH-165
TCH-165 is an enhancer of 20S proteasome assembly. TCH-165 regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation. TCH-165 enhances the proteolytic activity of the 20S proteasome by increasing substrate accessibility to the 20S catalytic chamber through 20S gate opening. TCH-165 enhances 20S-mediated degradation of IDPs, α-syn, and tau in vitro, and does not induce the degradation of structured proteins such as GAPDH. TCH-165 enhances c-MYC degradation by the 20S proteasome, which reduces c-MYC levels in vivo, and is effective in bortezomib (Cat. No. 7282) resistant cells. TCH-165 down-regulates c-MYC target genes and inhibits cancer cell proliferation and tumor growth in vivo.
Technical Data for TCH-165
|Storage||Store at -20°C|
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 TCH-165
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TCH-165
The following data is based on the product molecular weight 595.74. 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||1.68 mL||8.39 mL||16.79 mL|
|5 mM||0.34 mL||1.68 mL||3.36 mL|
|10 mM||0.17 mL||0.84 mL||1.68 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References for TCH-165
References are publications that support the biological activity of the product.
Azevedo et al (2013) Inhibition of the human proteasome by imidazoline scaffolds. J.Med.Chem. 56 10.1021 PMID: 23789888
Njomen et al (2020) Enhancing c-MYC degradation via 20S proteasome activation induces in vivo anti-tumor efficacy. BioRxiv- not yet peer reviewed
Njomen et al (2018) Small molecule modulation of proteasome assembly. Biochemistry 57 4214 PMID: 29897236
If you know of a relevant reference for TCH-165, please let us know.
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Keywords: TCH-165, TCH-165 supplier, TCH165, enhancers, enhances, 20S, proteasomes, assembly, modulators, activators, c-myc, Proteasome, 7489, Tocris Bioscience
Citations for TCH-165
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Literature in this Area
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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
- TAG Degradation Platform
- Degrader Building Blocks
- Custom Degrader Services
- Ubiquitin-Proteasome System Proteins and Assays
- Assays for 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. Presented at EFMC 2018, Ljubljana, Slovenia