IndraLab

Statements

VLX1570 inhibits UCHL5. 11 / 11
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"VLX1570 is known to induce apoptosis of myeloma by targeting USP4 and UCHL5 [XREF_BIBR]."
32486158
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"VLX1570, a small molecule DUB inhibitor derived from b-AP15 [(3E,5E)-3,5-bis[(4-nitrophenyl)methylidene]-1-(prop-2-enoyl)piperidin-4-one], selectively inhibits USP14 and UCHL5, which are associated with the 19S regulatory subunit of the proteasome."
40001543
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"A similar phenomenon is seen with b-AP15 and VLX1570 that are reported to inhibit the proteasomal DUBs UCH37 and USP14."
37315065
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"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
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"67 In 2015, a selective inhibitor of USP14/UCHL5, VLX1570, was approved for a phase I/II clinical trial in patients with multiple myeloma (NCT02372240)."
35760282
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"VLX1570( 7p ) can specifically block the activity of USP14 and UCHL5, causing rapid accumulation of high molecular weight ubiquitin conjugates, showing strong anti-tumor activity."
34974338
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"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
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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)."
30851297
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"VLX1570, a derivative of b-AP15, was identified to inhibit proteasome DUBs (including USP14 and UCHL5) activity in vitro in a manner consistent with competitive inhibition [ 75 ]."
31676235
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"VLX1570 is an inhibitor of USP14 and UCHL5 with apoptosis-inducing and antineoplastic activities [117] ."
29864528
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"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