SML3911
TCH-165
≥98% (HPLC)
别名:
Ethyl (4R,5R)-rel-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate, rel-Ethyl (4R,5R)-4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-1H-imidazole-4-carboxylate
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生化／生理作用
Cell-permeable and potent activator of 20S proteasome assembly that and enhances 20S-mediated proteolysis.
TCH-165 is a cell-permeable and potent activator of 20S proteasome assembly that favors a proteolytically active, open-gate 20S proteasome subcomplex and enhances 20S-mediated proteolysis (nearly 10-fold ≤1.5 µM) to the detriment of the 26S proteasome, in a time- and dose-dependent manner. TCH-165 restores proteostasis and enhances degradation of intrinsically disordered proteins (IDPs) both in purified protein assays and in cell culture (α-synuclein, tau441, c-MYC, cFos, ornithine decarboxylase). TCH 165 degrades SNAP29 and syntaxin 17 and reduces autophagosome-lysosome fusion. TCH165 inhibits cancer cell proliferation, impedes in vivo tumor growth, and offers neuroprotection from distinct dipeptide repeat (DPR) protein toxicity and is well tolerated in vivo (in mice and in dogs) at therapeutic concentrations.
TCH-165 is a cell-permeable and potent activator of 20S proteasome assembly that favors a proteolytically active, open-gate 20S proteasome subcomplex and enhances 20S-mediated proteolysis (nearly 10-fold ≤1.5 µM) to the detriment of the 26S proteasome, in a time- and dose-dependent manner. TCH-165 restores proteostasis and enhances degradation of intrinsically disordered proteins (IDPs) both in purified protein assays and in cell culture (α-synuclein, tau441, c-MYC, cFos, ornithine decarboxylase). TCH 165 degrades SNAP29 and syntaxin 17 and reduces autophagosome-lysosome fusion. TCH165 inhibits cancer cell proliferation, impedes in vivo tumor growth, and offers neuroprotection from distinct dipeptide repeat (DPR) protein toxicity and is well tolerated in vivo (in mice and in dogs) at therapeutic concentrations.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Small Molecule Modulation of Proteasome Assembly
Biochemistry, 57(28), 4214-4224 (2018)
Enhanced Degradation of Mutant C9ORF72-Derived Toxic Dipeptide Repeat Proteins by 20S Proteasome Activation Results in Restoration of Proteostasis and Neuroprotection
ACS Chemical Neuroscience (2023)
Evert Njomen et al.
Cell chemical biology, 26(9), 1283-1294 (2019-07-23)
The proteolytic arm of the protein homeostasis network is maintained by both the ubiquitin-proteasome system (UPS) and autophagy. A well-balanced crosstalk between the two catabolic pathways ensures energy-efficient maintenance of cellular function. Our current understanding of the crosstalk between the
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