1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. DNA Alkylator/Crosslinker

DNA Alkylator/Crosslinker

DNA alkylator/crosslinker is a molecule that alkylates DNA or can cross link with DNA. DNA alkylator/crosslinker can have mutagenic, pharmaceutical, or other effects. Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene. Alkylating agents are widely used in chemistry because the alkyl group is probably the most common group encountered in organic molecules. Selective alkylation, or adding parts to the chain with the desired functional groups, is used, especially if there is no commonly available biological precursor. Alkylation with only one carbon is termed methylation. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Crosslinking of DNA occurs when various exogenous or endogenous agents react with two different positions in the DNA. This can either occur in the same strand (intrastrand crosslink) or in the opposite strands of the DNA (interstrand crosslink). Crosslinks also occur between DNA and protein. DNA replication is blocked by crosslinks, which causes replication arrest and cell death if the crosslink is not repaired. The RAD51 family plays a role in repair.

DNA Alkylator/Crosslinker Related Products (54):

Cat. No. Product Name Effect Purity
  • HY-17394
    Cisplatin >99.0%
    Cisplatin (CDDP) is an antineoplastic chemotherapy agent by cross-linking with DNA and causing DNA damage in cancer cells. Cisplatin activates ferroptosis and induces autophagy.
  • HY-17371
    Oxaliplatin 99.86%
    Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
  • HY-17364
    Temozolomide 99.98%
    Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
  • HY-17393
    Carboplatin 99.93%
    Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.
  • HY-17420
    Cyclophosphamide >98.0%
    Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.
  • HY-117433
    4-Hydroperoxy cyclophosphamide
    4-Hydroperoxy cyclophosphamide is the active metabolite form of the prodrug Cyclophosphamide. 4-Hydroperoxy cyclophosphamide crosslinks DNA and induces T cell apoptosis independent of death receptor activation, but activates mitochondrial death pathways through production of reactive oxygen species (ROS). 4-Hydroperoxy cyclophosphamide is used to treat lymphomas and autoimmune disorders.
  • HY-124325
    PIP-199 >98.0%
    PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
  • HY-105019A
    Melflufen hydrochloride 98.23%
    Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
  • HY-13753
    Streptozocin 99.58%
    Streptozocin is a potent DNA-methylating antibiotic. Streptozotocin causes methylation of liver and kidney and pancreatic DNA, but no methylation in brain DNA.
  • HY-17419
    Ifosfamide >98.0%
    Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
  • HY-19609
    Calicheamicin 98.44%
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.
  • HY-B0245
    Busulfan >98.0%
    Busulfan is a potent alkylator with selective immunosuppressive effect on bone marrow.
  • HY-16293
    Lurbinectedin 99.73%
    Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
  • HY-17420A
    Cyclophosphamide hydrate >98.0%
    Cyclophosphamide hydrate is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.
  • HY-13424
    RITA 99.57%
    RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.
  • HY-B0077
    Bendamustine hydrochloride 98.00%
    Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
  • HY-13669
    Lomustine 99.91%
    Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.
  • HY-13585
    Carmustine 99.85%
    Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA.
  • HY-17574
    Thio-TEPA >98.0%
    Thio-TEPA is a DNA alkylating agent, with antitumor activity.
  • HY-13733
    Procarbazine Hydrochloride
    Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
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