IndraLab

Statements


VLX1570 activates USP14. 2 / 2
| 2

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"Notwithstanding this success, the potency of pimozide (IC50 ~2 μM) is lower than those of clinically approved UPS inhibitor 26S proteasome inhibitor Bortezomib (IC50 ~100 nM) (Fig. 1 and Table 2), and another UPS inhibitor VLX1570, which inhibited the DUBs UCHL5 and USP14 (IC50 ~100 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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"Indeed, VLX1570 preferentially targets USP14 and exhibits selective cytotoxicity in MM cells, which have a high expression of USP14 [XREF_BIBR]."