Cuproptosis Inducer

Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu²⁺ increases intracellular ROS levels and induces cuproptosis.

Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research.

Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu²⁺ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer.

Zinc Pyrithione is an antifungal and antibacterial agent disrupting membrane transport by blocking the proton pump. Zinc Pyrithione is also a copper ionophore that delivers copper into cells and is a useful tool for studying cuproptosis.

Antitumor photosensitizer-10 is an antitumor photosensitizer. Upon near-infrared irradiation, Antitumor photosensitizer-10 generates superoxide anions, reduces the copper-binding capacity of glutathione, releases copper ions, and thereby induces cuproptosis in tumor cells (cuproptosis). Antitumor photosensitizer-10 can be used in breast cancer-related research.

Disulfiram (Standard) is the analytical standard of Disulfiram. This product is intended for research and analytical applications. Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram + Cu²⁺ increases intracellular ROS levels triggering apoptosis of ovarian cancer stem cells^[1-6].

UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia.

Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC₅₀ values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.

Copper ionophore I is an efficient copper ion carrier. Copper ionophore I can regulate various intracellular copper levels to induce cuproptosis, such as 4T1 (IC₅₀ = 0.45 μM) and MDA-MB-231(IC₅₀ = 1.21 μM) cells. Copper ionophore I can induce an increase in ROS and cause mitochondrial dysfunction. Copper ionophore I can reduce the expression of FDX1, DLAT, and LIAS proteins. Copper ionophore I can activate immune related pathways and promote T cell infiltration. Copper ionophore I can be used for cancer research.

Zinc Pyrithione (Standard) is the analytical standard of Zinc Pyrithione. This product is intended for research and analytical applications. Zinc Pyrithione is an antifungal and antibacterial agent disrupting membrane transport by blocking the proton pump. Zinc Pyrithione is also a copper ionophore that delivers copper into cells and is a useful tool for studying cuproptosis.

PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC₅₀ of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.

DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate is an orally active prodrug of MMB-DTCs-1,3-diaminopropane-DTCs-MMB (HY-182917). DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate induces apoptosis, ferroptosis, and cuproptosis in lung cancer cells. DMAPT-DTCs-1,3-diaminopropane-DTCs-DMAPT dimethanesulfonate can be used in the research of lung cancer.

Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D is a copper ion carrier that can induce cuproptosis in triple-negative breast cancer cells by targeting PRDX1. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer.