TCH-165

Key Product Details

Product Description

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.

Product Specifications for TCH-165

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Njomen Enhancing c-MYC degradation via 20S proteasome activation induces in vivo anti-tumor efficacy. BioRxiv- not yet peer reviewed
• Njomen Small molecule modulation of proteasome assembly. Biochemistry 2018 PMID: 29897236
• Azevedo Inhibition of the human proteasome by imidazoline scaffolds. J.Med.Chem. 2013 PMID: 23789888

Product Documents for TCH-165