Chemical Name: Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
Biological ActivityTCH-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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