p97

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.

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

MSC1094308 is a reversible, non-ATP-competitive alterative inhibitor targeting type II AAA ATPase (VCP/p97) and type I AAA ATPase (VPS4B), which affects the intracellular protein degradation process by binding to a specific hotspot region of p97 and inhibiting D2 ATPase activity.

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

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

VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with an IC50 of 32 nM for p97. It exhibits excellent antitumor activity, significantly suppressing tumor growth in a Molm-13 xenograft mouse model. VCP/p97 IN-2 is applicable for research in acute myeloid leukemia (AML).

p97-IN-1 is an orally active inhibitor of p97 with an IC50 of 26 nM. It significantly impedes the proliferation of tumor cells and is applicable for research in acute myeloid leukemia (AML).

ML241 is a potent and selective inhibitors of p97 ATPase.

ML240 is a selective, ATP-competitive p97 inhibitor.

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).

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

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

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

VCP/p97 IN-3 is an allosteric inhibitor of VCP/p97. It exhibits inhibitory activity against VCP, with an IC50 of 9 nM, and shows IC50 values of 12 nM (N660K) and 19 nM (V474A/D649A) for mutant VCP proteins. VCP/p97 IN-3 increases the levels of K48 ubiquitination and caspase-3. It activates endoplasmic reticulum stress and the unfolded protein response (UPR). In a subcutaneous xenograft mouse model with RPMI-8226 cells, VCP/p97 IN-3 suppresses tumor growth. This compound is applicable for research in multiple myeloma.

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.

UPCDC30245 is an AAA ATPase p97 allosteric inhibitor.

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.

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.

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.

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

UP12 enhances ATPase activity by activating valosin-containing protein (VCP), with an EC50 of 2.57 μM.

UP163 enhances ATPase activity and activates valosin-containing protein (VCP), with an EC50 of 9.0 μM. It also reduces MG-132-induced TDP-43 aggregation.

UP158 enhances ATPase activity and stimulates valosin-containing protein (VCP), with an EC50 of 2.57 μM.