cuproptosis

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

UM4118 (N-quinolin-8-ylpyridine-2-carboxamide) is a copper ion carrier that triggers an atypical form of mitochondria-based cell death (cuproptosis).UM4118 can be used for the study of acute myeloid leukemia.UM4118 showed no significant effect on VEGF and b-FGF stimulated HMVEC proliferation with LC values of 0.013 and 0.018 μM, respectively.

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15/1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

Tiomolibdate diammonium (NSC-286644) is an inhibitor of superoxide dismutase 1 (SOD1) exerting antiangiogenic and antitumor activities. Tiomolibdate diammonium inhibits the activities of cuproenzymes, including SOD1 and COX.

Zinc pyrithione (OM-1563), an antibacterial and antifungal agent can disrupt membrane transport by blocking the proton pump.

Emeramide (BDTH2) is a thiol-redox antioxidant. It is also a heavy metal chelator.

Tetrathiomolybdate (TM) promotes the dimerization of the metal-binding domain (WLN4) of the cellular copper efflux protein ATP7B through its characteristic sulfur bridge Mo2S6O2 cluster, and is used in the clinical treatment of Wilson's disease.

Cu(II)-Elesclomol is a complex formed by the anticancer agent Elesclomol and Cu(II), which selectively transports copper to mitochondria.Cu(II)-Elesclomol has anticancer activity, inhibits the growth of human leukemia K562 cells, and induces cell-cycle arrest, and is used in the study of leukemias.

NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].