IndraLab

Statements


UPS inhibitor inhibits USP14. 2 / 2
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"Notwithstanding this success, the potency of pimozide (IC 50~2 μM) is lower than those of clinically approved UPS inhibitor 26S proteasome inhibitor Bortezomib (IC 50~1 00 nM) ( Fig. 1 and Table 2 ), and another UPS inhibitor VLX1570, which inhibited the DUBs UCHL5 and USP14 (IC 50~1 00 nM) and was previously studied in clinical trials but terminated due to limiting toxicities (study identifier NCT02372240) (ClinicalTrials.gov, 2018; Wang et al., 2016) ."

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"Notwithstanding this success, the potency of pimozide (IC 50 ~ 2muM) is lower than those of clinically approved UPS inhibitor 26S proteasome inhibitor Bortezomib (IC 50 ~ 100nM) (XREF_FIG and XREF_TABLE), and another UPS inhibitor VLX1570, which inhibited the DUBs UCHL5 and USP14 (IC 50 ~ 100nM) and was previously studied in clinical trials but terminated due to limiting toxicities (study identifier NCT02372240)."