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 .