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You are here:Home-Inhibitors & Agonists-Proteasome/Ubiquitin-p97/VCP

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p97 is an abundant hexameric ATPase of the AAA family, is involved in homotypic membrane fusion. It is thought to disassemble SNARE complexes formed during the process of membrane fusion. Two structures have been reported: a crystal structure of the N-terminal and D1 ATPase domains of murine p97 at 2.9 A resolution, and a cryoelectron microscopy structure of full-length rat p97 at 18 A resolution. Together, these structures show that the D1 and D2 hexamers pack in a tail-to-tail arrangement, and that the N domain is flexible. A comparison with NSF D2 (ATP complex) reveals possible conformational changes induced by ATP hydrolysis.

Cat. No. Product Name CAS No. Information
H7256

UPCDC30245

1883351-01-6

UPCDC30245 is an allosteric inhibitor of AAA ATPase p97 with IC50 of 27 nM, binds at the junction between the D1 and D2 domains of p97.

H7255

NPD8733

696655-62-6

NPD8733 (NPD-8733) is a small-molecule ligand of valosin-containing protein (VCP)/p97, binds to the D1 domain of VCP/p97; suppresses the enhanced migration of NIH3T3 cells co-cultured with MCF7 cells using a wound healing co-culture assay.

H7254

MSC 1094308

2219320-08-6

MSC1094308 (MSC 1094308) is a reversible, allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B with IC50 of 7.2 and 0.71 uM, respectively; binds to drugable hotspot of p97, thereby inhibiting the D2 ATPase activity; is active in cells, and specifically inhibits p97 but not the proteasome.

H7253

ML-241 hydrochloride

2070015-13-1

ML241 Hcl is a potent, selective and reversible AAA ATPase p97 inhibitor (IC50=100 nM); blocks degradation of p97-dependent proteasome substrate with an IC50 of 3.5 uM; induces caspases 3 and 7 and potently blocks proliferation in HCT15 and SW403 cells.

H7252

ML-241

1346528-06-0

ML241 is a potent, selective and reversible AAA ATPase p97 inhibitor (IC50=100 nM); blocks degradation of p97-dependent proteasome substrate with an IC50 of 3.5 uM; induces caspases 3 and 7 and potently blocks proliferation in HCT15 and SW403 cells.

H7251

ML-240

1346527-98-7

ML240 is a potent, selective and reversible AAA ATPase p97 inhibitor (IC50=100 nM); blocks degradation of p97-dependent proteasome substrate with an IC50 of 0.9 uM; induces caspases 3 and 7 and potently blocked proliferation in HCT15 and SW403 cells.

H7250

LC-1028

2324158-08-7

LC-1028 (LC1028) is a novel potent selective, covalent and irreversible inhibitor of p97 (valosin-containing protein), remains essentially irreversible ac tivity against p97 mutant C522A.

H7249

CB-5083

1542705-92-9

CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3; causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and generation of irresolvable proteotoxic stress, leading to activation of the apoptotic arm of the unfolded protein response (UPR) in cancer cells; inhibits A549 cell viability with IC50 of 0.67 uM, induces the UPR and apoptosis in xenograft tumor models.

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