TCH-165
Tocris Bioscience, part of Bio-Techne | Catalog # 7489
Enhancer of 20S proteasome assembly and 20S-mediated protein degradation
Key Product Details
Description
Enhancer of 20S proteasome assembly and 20S-mediated protein degradation
Alternative Names
TCH165
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
Molecular Weight
595.74
Formula
C39H37N3O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
CAS Number
1446350-60-2
PubChem ID
71762768
InChI Key
XXDLWRCUPASJGY-AEGYFVCZSA-N
SMILES
CCOC([C@@]1(C2=CC=CC=C2)[C@@H](C3=CC=C(C=C3)NCC4=CC=CC=C4)N(C(C5=CC=C(C=C5)OC)=N1)CC6=CC=CC=C6)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 59.57 | 100 | |
| Ethanol | 59.57 | 100 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for TCH-165
For research use only
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