DNA interstrand cross-links

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Nedaplatin (NSC-375101D) is a derivative of cisplatin and DNA damage agent for tumor colony forming units (IC50: 94 μM). Containing a novel ring structure in which glycolate is bound to the platinum by a bidentate ligand, nedaplatin forms reactive platinum complexes that bind to nucleophilic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death.

SG3199 is a PBD dimer which binds in the minor groove of DNA, and forms covalent DNA interstrand cross-links in naked linear plasmid DNA. SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines.

Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.

Porfiromycin is a n N-methyl derivative of the antineoplastic antibiotic mitomycin C isolated from the bacterium Streptomyces ardus and other Streptomyces bacterial species. Bioreduced porfiromycin generates oxygen radicals and alkylates DNA, producing interstrand cross-links and single-strand breaks, thereby inhibiting DNA synthesis. Porfiromycin is preferentially toxic to hypoxic cells.

Caricotamide is a synthetic co-substrate that activates the human endogenous enzyme NRH:quinone oxidoreductase 2 (NQO2) with potential chemoadjuvant activity. When caricotamide is administered simultaneously with the prodrug tretazicar, NQO2 converts tretazicar to the bifunctional alkylating agent dinitrobenzamide, which is capable of forming a high degree of DNA interstrand cross-links, resulting in the inhibition of DNA replication and the induction of apoptosis. NQO2 has been found to be over-expressed in cancers such as hepatocellular carcinoma (HCC), colorectal and ovarian cancers.

Colibactin 742, a stable derivative of colibactin, efficiently induces DNA interstrand cross-links, activates the Fanconi Anemia DNA repair pathway, and leads to G2/M arrest.

Olintatug (ADCT-901) is a highly specialized antibody-drug conjugate (ADC) targeting Kidney-Associated Antigen 1 (KAAG1). It comprises a humanized monoclonal antibody conjugated to a potent pyrrolobenzodiazepine (PBD) dimer cytotoxin via a cathepsin-cleavable linker. Olintatug specifically binds to KAAG1 on tumor cell surfaces, internalizes, and releases the PBD dimer, which induces lethal DNA interstrand cross-links, blocking cell division. It is investigated for KAAG1-expressing solid tumors, including ovarian and triple-negative breast cancers.

Trioxsalen (Standard) is the standard substance of Trioxsalen, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Trioxsalen (Trioxysalen) is a furanocoumarin and a psoralen derivative, in conjunction with UV-A for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death.