IndraLab

Statements

VLX1570 inhibits USP14. 8 / 8
| 8
reach
"b-AP15/VLX1570 are small molecule inhibitors of the ubiquitin specific peptidase 14 (USP14) and ubiquitin carboxyl-terminal hydrolase 5 (UCHL5) deubiquitinases (DUBs) of the 19S proteasome."
31639138
reach
"Preferential inhibition of USP14 by VLX1570."
27264969
reach
"The small molecule VLX1570 and an analog b-AP15 specifically block the activity of DUBs USP14 and UCHL5 in the 19S regulatory subunit, which results in the rapid accumulation of high molecular weight ubiquitin conjugates, proteasome shutdown, and robust anti-tumor activity in well established orthotopic and xenograft models of MM, lymphoma, Ewing 's sarcoma, and other malignancies [XREF_BIBR - XREF_BIBR]."
32125598
reach
"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)."
30851297
reach
"VLX1570 was indeed found to inhibit USP14 in cells at a concentration of 1 mum (XREF_FIG)."
25854145
reach
"VLX1570 and b-AP15 both inhibit USP14 and UCHL5 activity of 19S regulatory particles with the inhibition of USP14 being more pronounced (XREF_FIG)."
25854145
reach
"Results suggested an increased inhibition of USP14 by VLX1570 compared with b-AP15."
32272746
reach
"We observed at 30min that VLX1570 inhibited the activity of both USP14 and UCHL5 in a manner similar to b-AP15, as noted by a decrease in UbVS labeled DUBs (XREF_FIG)."
27813535