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UPCDC-30766 (UPCDC 30766) is a potent, allosteric inhibitor of AAA+ ATPase p97 (valosin-containing protein, VCP) with biochemical IC50 of 12 nM, EC50 of 226 nM in cellular UbG76V-GFP accumulation assays.
OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).
VCP Activator 1 (VA1) is a small molecule allosteric activator of valosin-containing protein (VCP)/p97, dose-dependently stimulates VCP ATPase activity up to 3-fold (EC50= 4 uM).
UPCDC-30766 (UPCDC 30766) is a potent, allosteric inhibitor of AAA+ ATPase p97 (valosin-containing protein, VCP) with biochemical IC50 of 12 nM, EC50 of 226 nM in cellular UbG76V-GFP accumulation assays.
NW1030 is a small molecule that target the regulatory domain of VCP/p97, increases the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.
NW1028 is a small molecule that target the regulatory domain of VCP/p97, inhibits the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.
FL-18 (p97 inhibitor FL-18) is is the first small-molecule covalent inhibitor of VCP/p97 AAA ATPase with IC50 of 59.3 nM, capable of covalent engagement of p97 with proteome-wide selectivity.FL-18 showed better inhibition potency than NMS-873, a well-known p97 inhibitor.FL-18 covalently modified C522 residue in p97 and showed potent enzymatic inhibition.FL-18 showed potent inhibition towards U87MG glioma cancer cells (IC50=31 nM).FL-18 inhibited the p97 activity and induced aggregation of ubiquitinated proteins in U87MG cells.
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