p97

WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively inhibited the in vitro invasiveness of EGFR-positive human cancer cells in a concentration-dependent manner.

WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.

VCP/p97 inhibitor-1, a highly effective compound, inhibits VCP/p97 (also known as Cdc48, CDC-48, or Ter94) with an IC 50 of 54.7 nM. This inhibitor induces a disruption in protein homeostasis and interferes with the degradation process of misfolded polypeptides by the ubiquitin-proteasome system (UPS).

ATPγS tetralithium salt is a substrate for nucleotide hydrolysis and RNA unraveling activity of the eukaryotic translation initiation factor eIF4A, associated with p97 mutants and prions.

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).

UPCDC30245 is an AAA ATPase p97 allosteric inhibitor.

NMS-873 is a potent, selective allosteric VCP/p97 inhibitor.

NPD8733 is an inhibitor of cancer cell-enhanced fibroblast migration. It specifically binds to valosin-containing protein (VCP)/p97.

SMDC818909 is an effective and selective p97 inhibitor.

MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

LC-1310 is an irreversible p97 inhibitor.

ML240 is a selective, ATP-competitive p97 inhibitor.

UPCDC30766, a potent allosteric inhibitor of p97, exhibits an IC50 of 12 nM and is applicable for colon cancer research [1].

LC-1028 is a novel potent selective, covalent and irreversible inhibitor of p97 (valosin-containing protein) with IC50 =33 nM.

MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase.

NMS-859 is an effective and covalent inhibitor of valosin-containing protein (VCP)/p97 with IC50s of 0.37 μM and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively.

NW 1028 is a potent inhibitor of VCP/p97. NW 1028 selectively acts on the ND1L domain of p97 and inhibits the degradation of p97-dependent reporter genes. NW 1028 has a regulatory effect on the mitotic spindle.

Eeyarestatin I is an inhibitor that inhibits the degradation and translocation of ER-associated proteins. Eeyarestatin I is associated with the p97 deubiquitination process and inhibits atx3 deubiquitination. Eeyarestatin I has anticancer effects by inducing proteins that cause cell death.

ML241 is a potent and selective inhibitors of p97 ATPase.ML241 inhibits degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. ML241 may be a novel agent for the chemotherapy of cancer, and provide a rationale for developing pathway-specific p97 inhibitors.

ML241 is a potent and selective inhibitors of p97 ATPase.

ACJI-99C is a cell-permeable irreversible Cdc48/p97 inhibitor.

p97-IN-1 is a potent inhibitor of p97 with an IC 50 <30 nM [1].

DBEQ (JRF 12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor.