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DNA Alkylator/Crosslinker

DNA alkylator/crosslinker is a molecule that alkylates or can crosslink DNA. Alkylation is a chemical reaction that entails the transfer of an alkyl group. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effecting alkylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with a class of drugs called alkylating antineoplastic agents.

  • Cisplatin
    T156415663-27-1
    Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.
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    • $28
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  • Temozolomide
    T117885622-93-1
    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.
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  • Oxaliplatin
    T016461825-94-3
    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.
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  • Streptozocin
    T150718883-66-4
    Streptozocin (NSC-85998) is an antibiotic that induces DNA methylation. Streptozocin is toxic to insulin-producing pancreatic islet B-cells and is commonly used in the construction of animal models of type 1 diabetes. The product is unstable in solution and is recommended to be dispensed now.
    • $30
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  • N-Nitroso-N-methylurea
    T4169684-93-5
    N-Nitroso-N-methylurea is a nitrosourea compound with alkylating, carcinogenic and mutagenic properties. It targets a variety of animal organs, causes various cancers and degenerative diseases, and can be used in diazomethane synthesis.
    • $36
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  • Illudin M
    T365281146-04-9
    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.
    • $533
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  • Semustine
    T1687113909-09-6In house
    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.
    • $138
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  • Carmustine
    T3091154-93-8
    Carmustine (bis-chloroethylnitrosourea) is a cell-cycle phase nonspecific alkylating antineoplastic agent.
    • $40
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  • Carboplatin
    T105841575-94-4
    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.
    • $36
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  • PK11000
    T445938275-34-2
    PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.
    • $33
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  • RITA
    T1798213261-59-7
    RITA (NSC-652287)(NSC-652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53/Mdm2 interaction.
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  • Bendamustine hydrochloride
    T00953543-75-7
    Bendamustine hydrochloride (EP-3101) (IC50 of 50 μM) is an alkylating agent associated with DNA damage.
    • $43
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  • Cyclophosphamide hydrate
    T07076055-19-2
    Cyclophosphamide hydrate is a DNA alkylating agent, an inhibitor of DNA synthesis. Cyclophosphamide hydrate has antitumor and immunosuppressive activities.
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  • Illudin S
    T228571149-99-1
    Illudin S (ILS) is a fungal sesquiterpene secondary metabolite with potent genotoxic and cytotoxic properties.
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  • VAL-083
    T1721223261-20-3
    VAL-083 is an alkylating agent with antitumor activity that produces N7 methylation on DNA.
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  • Miriplatin
    T4368141977-79-9
    Miriplatin (SM-11355) (SM-11355) is a platinum complex used in TACE that has promise for the therapy of hepatocellular carcinoma (HCC).
    • $41
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  • Pipobroman
    T457054-91-1
    Pipobroman (Vercyte) is an anti-cancer drug that probably acts as an alkylating agent. Pipobroman has well documented clinical activity in polycythemia vera (PV) and essential thrombocythemia (ET). Pipobroman allows, within 3 months, to attain a response in more than 90% of patients, without clinically relevant toxicities. The 10-years risk of thrombosis of patients treated with Pipobroman is about 15%, The anti-proliferative activity of Pipobroman on bone marrow megakaryocytes seems of particular value in lowering the occurrence of post-PV and post-ET MMM, whose risk is the lowest registered with available treatments. The 10-year risk of acute leukemia with Pipobroman is 5% in PVand 3% in ET, which is only slightly higher than that expected as a natural evolution of the disease. In conclusion, the use of Pipobroman is a definite alternative to hydroxyurea in patients with PV and ET at high risk of thrombosis.
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  • Trioxsalen
    T45583902-71-4
    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.
    • $29
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  • Tretazicar
    T679821919-05-1
    CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.
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  • Ifosfamide
    T10553778-73-2
    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.
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  • Altretamine
    T1241645-05-6
    Altretamine (ENT-50852) is an alkylating agent with antineoplastic activity.
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  • KCC-07
    T8554315702-75-1
    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
    • $34
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  • Cyclophosphamide
    T0707L50-18-0
    Cyclophosphamide is an alkylating agent used in the treatment of several forms of cancer including leukemias, lymphomas and breast cancer.
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  • Busulfan
    T092355-98-1
    Busulfan (Busulphan) is a synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription.
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  • Thio-TEPA
    T125052-24-4
    Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.
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  • Satraplatin
    T7221129580-63-8
    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.
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  • Chlorambucil
    T0975305-03-3
    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.
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  • Lomustine
    T160113010-47-4
    Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.
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  • Nimustine Hydrochloride
    T501755661-38-6
    Nimustine Hydrochloride (Nidran hydrochloride) has been used in trials studying the treatment of Glioblastoma.
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  • Procarbazine hydrochloride
    T1488366-70-1
    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.
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  • Palifosfamide
    T435031645-39-3
    Palifosfamide (Isophosphamide mustard) lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma lines in vitro. The IC50 ranges from 2.25 to 6.75 μM for most cell lines except OS222 (IC50=31.5 μM).
    • $70
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  • Treosulfan
    T17159299-75-2
    Treosulfan (Treosulphan) is a bifunctional alkylating agent. It also has activity in ovarian cancer and other solid tumor types.
    • $34
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  • Bendamustine
    T838016506-27-7
    Bendamustine (SDX105) for the treatment of Non-Hodgkin Lymphomas and Chronic Lymphocytic Leukemia
    • $32
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