dna-crosslinking

6-Aminonicotinamide (6-AN) is a well-established inhibitor of the NADP+-dependent enzyme.

MC-Val-Ala-PBD is a drug-linker conjugate for ADC by using the antitumor antibiotic, pyrrolobenzodiazepine (PBD, a cytotoxic DNA crosslinking), linked via the cleavable linker MC-Val-Ala[1].

Amotosalen hydrochloride (S-59) is a light-activated, RNA- and DNA-crosslinking psoralen compound used to neutralize pathogens.

Metamelfalan is an alkylating nitrogen mustard with potential antineoplastic activity. It causes crosslinking of DNA, thereby preventing DNA replication and eventually cellular proliferation.

Ametantrone Acetate is a topoisomerase II inhibitor of anthrapyrazole family, which can lead to DNA covalent crosslinking.

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)

EC2629 is a highly potent DNA crosslinking agent targeting the folate receptor.

Bisantrene (CL216942) is an anthracenyl bishydrazone with antineoplastic activity. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity.

(rel)-Oxaliplatin, a DNA synthesis inhibitor, induces DNA crosslinking damage, inhibits DNA replication and transcription, and stimulates apoptosis. This compound has applications in cancer research [1] [2] [3].

Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2.7 µM, respectively). It reduces tumor growth in an HCCLM3 mouse xenograft model when administered at doses of 5 or 10 mg kg once per week. Formulations containing oxaliplatin have been used in the treatment of advanced colorectal cancer and as adjuvants in stage III colon cancer.

Busulfan-d8 (Sulphabutin-d8) is a deuterated Busulfan. Busulfan is an effective alkylating anticancer agent with immunosuppressive and myeloablative activities. It exerts anti-cancer activity by crosslinking DNA and causing DNA damage.