IMP-2373

IMP-2373 (8 h; 24 h) shows no cytotoxicity against T47D, U2OS and U87-MG cells after 8 h of treatment, and exhibits only extremely low cytotoxicity after 24 h of treatment, with EC₅₀ values all higher than 60 μM in these three cell lines^[1].
IMP-2373 (10 μM; 1 h) is a competitive probe that selectively and efficiently detects the target engagement of intracellular active DUB inhibitors, including the UCHL1 inhibitor IMP-1711-S and the USP30 inhibitor FT385, in U87-MG and T47D cells^[1].
IMP-2373 (25 μM; 1 h) captures the activity of 38 deubiquitinases in P493-6 B-cell lymphoma cells, and reveals that dysregulation of oncogenic MYC drives global downregulation of DUB activity, which is independent of DUB abundance. Meanwhile, the activities of UCHL3, USP7, USP47, USP10 and ATXN3 are selectively upregulated in low-MYC cells^[1].
IMP-2373 exhibits extremely low off-target cytotoxicity: no reduction in cell viability is observed after treatment with >100 μM for 8 h in T47D and U2OS cells; no reduction in cell viability is detected either after treatment with 95.4 μM for 8 h in U87-MG cells; additionally, the 24 h EC₅₀ values range from 8.9 μM (U87-MG) to 86.5 μM (T47D)^[2].
IMP-2373 (10 μM; 1 h) acts as a competitive probe for the quantitative detection of intracellular target engagement corresponding to selective DUB inhibitors (UCHL1 and USP30 inhibitors) in U87-MG and T47D cells, respectively^[2].
Analysis of DUB activity changes in P493-6 B cell lymphoma cells treated with IMP-2373 (25 μM; 1 h) shows that global DUB activity is lower in high MYC cells, while UCHL3, USP7, USP47, USP10 and ATXN3 exhibit significantly higher activity relative to their abundance in low MYC cells^[2].

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