MT16-001 

MT16-001 is a cell-permeable UCHL1 inhibitor with an IC₅₀ 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^[1].

MT16-001 (30 min) potently inhibits recombinant UCHL1 (IC₅₀ = 580 nM) and USP30 at 1 μM, while showing no inhibition of recombinant UCHL3 at concentrations up to 10 μM^[1].
MT16-001 (72 h) exhibits cytotoxicity against HEK293 cells with an EC₅₀ of 730 nM^[1].
MT16-001 (1 h) engages UCHL1 in intact Cal51 cells stably expressing FLAG-UCHL1 with an IC₅₀ of 550 nM^[1].
MT16-001 (2-2000 nM; 3 h) causes no acute disruption of the whole proteome in HEK293 cells at concentrations up to 2000 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

298.36

C₁₅H₁₄N₄OS

1895049-73-6

O=C([C@@H]1CN(CC1)C#N)NC2=NC=C(C3=CC=CC=C3)S2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Panyain N, et al. Activity-based protein profiling reveals deubiquitinase and aldehyde dehydrogenase targets of a cyanopyrrolidine probe. RSC Med Chem. 2021;12(11):1935-1943. Published 2021 Aug 16.