DNA Alkylator/Crosslinker

Streptozotocin (Streptozocin, NSC-85998) is an antibiotic that enters pancreatic β-cells via the glucose transporter (GLUT2) and induces DNA methylation, leading to β-cell apoptosis. It is toxic to insulin-producing cells and commonly used to establish diabetic animal models. This product is unstable in solution and is recommended to be prepared freshly before use.

Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Cyclophosphamide is a synthetic alkylating agent chemically related to nitrogen mustards. It possesses antitumor and immunosuppressive activities and is widely used in the treatment of various cancers. Additionally, cyclophosphamide is commonly used to induce animal models of premature ovarian failure, bone marrow suppression, cystitis, overactive bladder, and myocarditis.

N-Nitroso-N-methylurea (NMU MNU NMH) is a nitrosourea compound with alkylating, carcinogenic, and mutagenic properties; as a direct-acting alkylating agent, it interacts with DNA and targets multiple animal organs to induce various cancers and degenerative diseases, and is commonly used to induce disease models such as gastric cancer and breast cancer in mice.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

KCC-07 is a selective, potent and brain-penetrant inhibitor of methyl-CpG-binding domain protein 2(MBD2) with anticancer activity. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti

Cyclophosphamide hydrate is a synthetic alkylating agent structurally related to nitrogen mustards, with antitumor and immunosuppressive activities. It is widely used in the treatment of various cancers and is also commonly employed to induce animal models of premature ovarian failure, myelosuppression, cystitis, and myocarditis.

4-hydroperoxy cyclophosphamide (4-OOH-CY) is an active metabolite of Cyclophosphamide that induces hepatotoxicity.4-Hydroperoxy cyclophosphamide increases levels of glutaminase and aspartate aminotransferase, enhances inflammatory factors and oxidative markers, and Inhibits oxidoreductase activity.4-Hydroperoxy cyclophosphamide is used in the study of cancer and autoimmune diseases.

Busulfan is an alkylating antineoplastic agent derived from dimethane sulfonate, with cytotoxic and immunosuppressive properties. It primarily acts by forming carbonium ions in vivo, which induce cross-linking between DNA strands or between DNA and proteins, leading to DNA damage, inhibition of DNA replication, and suppression of RNA transcription. In addition, Busulfan can inhibit thioredoxin reductase and induce apoptosis. It is commonly used as a myeloablative agent in preconditioning regimens for bone marrow transplantation and can also be used to establish anemia models.

Carmustine (bis-chloroethylnitrosourea) is a cell-cycle phase nonspecific alkylating antineoplastic agent.

Treosulfan (NSC 39069) is a bifunctional alkylating agent used in the treatment of advanced ovarian cancer.[2]

Illudin M is a cytotoxic sesquiterpene from the fungus O. illudens that alkylates DNA. It has a cytotoxicity of 6-100 nM against HL-60 human leukemia cells.Illudin M has anticancer activity and is a pre-drug for the synthesis of anticancer compounds.

Semustine, a DNA alkylating agent, is a cancer chemotherapy compound that is nephrotoxic in patients with malignant melanoma receiving adjuvant chemotherapy for the adjuvant treatment of leukemia.

Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.

Illudin S (ILS) is a fungal sesquiterpene secondary metabolite with potent genotoxic and cytotoxic properties.

Ifosfamide (NSC-109724) alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. Ifosfamide is a synthetic analog of the nitrogen mustard cyclophosphamide with antineoplastic activity. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

VAL-083 is an alkylating agent with antitumor activity that produces N7 methylation on DNA.

Bendamustine (SDX105) for the treatment of Non-Hodgkin Lymphomas and Chronic Lymphocytic Leukemia

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Satraplatin (BMS182751) is an orally available antineoplastic platinum(IV) complex.Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.

Chlorambucil (CB-1348) is an orally-active antineoplastic aromatic nitrogen mustard. Chlorambucil alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis.