TCH-165

Name: TCH-165
Brand: Tocris Bioscience
SKU: 7489

Tocris Bioscience, part of Bio-Techne | Catalog # 7489

COA / SDS

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
Chemical Name:	Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
Purity:	≥98% (HPLC)
Molecular Weight:	595.74

View Full Technical Details for TCH-165

Technical Data
Citations

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

M. Wt	595.74
Formula	C₃₉H₃₇N₃O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for TCH-165

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	59.57	100
	DMSO	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 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

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References for TCH-165

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