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.

Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity.

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 an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Duocarmycin TM is a DNA alkylator. Duocarmycin TM is an exceptionally potent antitumor antibiotic.

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.

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.

Calicheamicin (Calicheamicin γ1) is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.

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.

Phosphoramide mustard is a toxic metabolite of cyclophosphamide with anticancer activity and ovarian toxicity that induces DNA damage.

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

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.

Mitomycin C (Ametycine) is an antineoplastic agent and DNA double-strand crosslinking agent capable of inducing DNA damage, inhibiting DNA synthesis, suppressing mitosis, and activating apoptosis. Mitomycin C is a broad-spectrum antibiotic against both Gram-negative and Gram-positive bacteria.

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.

Iodoacetamide, an alkylating agent, is commonly utilized for cysteine alkylation in proteomics sample preparation.

Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.