1446350-60-2

TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation[1].

Cell-permeable and potent activator of 20S proteasome assembly th at and enhances 20S-mediated proteolysis.

TCH-165 is a cell-permeable and potent activator of 20S proteasome assembly th at favors a proteolytically activeopen-gate 20S proteasome subcomplex and enhances 20S-mediated proteolysis (nearly 10-fold ≤1.5 μM) to the detriment of the 26S proteasomein 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-synucleintau441c-MYCcFosornithine decarboxylase). TCH 165 degrades SNAP29 and syntaxin 17 and reduces autophagosome-lysosome fusion. TCH165 inhibits cancer cell proliferationimpedes in vivo tumor growthand offers neuroprotection from distinct dipeptide repe at (DPR) protein toxicity and is well tolerated in vivo (in mice and in dogs) at therapeutic concentrations.

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[1] Njomen E, et al. Small Molecule Modulation of Proteasome Assembly. Biochemistry. 2018 Jul 17;57(28):4214-4224. DOI:10.1021/acs.biochem.8b00579