p97 Inhibitor

VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC₅₀ of 9 nM and the mutant VCP proteins with IC₅₀ of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma.

p97-IN-1 is an orally active p97 inhibitor (IC₅₀ = 26 nM). p97-IN-1 can significantly inhibit the proliferation of tumor cells. p97-IN-1 can be used for research on acute myeloid leukemia (AML).

NSC804515 is an inhibitor of wild-type and R155H mutant p97/VCP ATPase, with an IC₅₀ of about 15 nM for both targets. NSC804515 acts as an antiproliferative agent, disrupts the function of the ubiquitin-proteasome system, induces UbG76V-GFP accumulation, and shows reduced inhibitory potency against p97 variants carrying P510S, K512N, N616F and F618S mutations. NSC804515 can be used in research related to cancer, inclusion body myopathy with early-onset Paget's disease and frontotemporal dementia, as well as familial amyotrophic lateral sclerosis.

NSC799462 is a triazole inhibitor of p97 ATPase. NSC799462 inhibits p97 ATPase activity (IC₅₀ = 15 nM) by binding to a specific site on p97 and causing local changes in the p97 structure.

LC-1310 is an antiviral agent that targets and inhibits p97, and it suppresses the in vitro replication of human cytomegalovirus (HCMV) with an EC₅₀ value of 0.3 μM. LC-1310 targets the D2 ATP-binding site of p97, downregulates the expression of early viral proteins, thereby blocking the transcription and proliferation of early viral genes. LC-1310 can be used for research on human cytomegalovirus infection.

p97-IN-2 (Compound 14) is a p97 ATPase (IC₅₀ = 0.6 μM) inhibitor. p97-IN-2 can inhibit cell proliferation, such as HCT15 (IC₅₀ = 1.1 μM) and SW403 (IC₅₀ = 0.8 μM) cells. p97-IN-2 can be used for cancer research.

Eeyarestatin I (Standard) is the analytical standard of Eeyarestatin I (HY-110078). This product is intended for research and analytical applications. Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.

ML240 (Standard) is the analytical standard of ML240. This product is intended for research and analytical applications. ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.

ACJI-99C (VCP/p97-IN-PPA) is a selective covalent p97/VCP ATPase inhibitor with an IC₅₀ value of 0.6 μM. ACJI-99C binds with p97 active site residues to block ATPase activity. ACJI-99C irreversibly blocks degradation of p97-dependent protein in cells. ACJI-99C inhibits proliferation of cancer cells, including p97 inhibitor-resistant lines. ACJI-99C can be used for the research of colorectal cancer.