MT16-001 is a cell-permeable UCHL1 inhibitor with an IC 50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30 , and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1 , and forms covalent interactions with ALDH2 , ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis.
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