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

DNA Alkylator/Crosslinker

DNA Alkylator/Crosslinker

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P991236
    MHES0488A
    MHES0488A is a selective humanized antibody that targets HER2 with a KD value of 0.8 nM. MHES0488A is an antibody part of DHES0815A. MHES0488A is internalized by cells and transported to lysosomes, and then releases PBD-monoamide that enters the nucleus, alkylates DNA and induces DNA damage and apoptosis. MHES0488A is promising for research of cancers, such as HER2-positive breast cancer and gastric cancer.
    MHES0488A
  • HY-19577
    Ambamustine
    Ambamustine (PTT119) is a new bifunctional alkylating agent and induces DNA damage by alkylating mechanisms. Ambamustine interferes with late steps in murine mammary tumor virus (MuMTV) processing and maturation and reduces production of the B-type retrovirus MuMTV. Ambamustine possesses cytolytic and antiviral activities.
    Ambamustine
  • HY-16406
    PR-104 sodium
    		Inhibitor
    PR-104 (sodium) is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104 (sodium), as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
    PR-104 sodium
  • HY-153851
    RNA Aptamer Peach Ⅱ sodium
    RNA Aptamer Peach Ⅱ (sodium) has an exceptionally high affinity to TO3-Biotin (TO3-B, red channel, ex: 637 nm, em: 658 nm), and can be used to visualize RNA expression or localization in live cells.
    RNA Aptamer Peach Ⅱ sodium
  • HY-139453A
    LP-284
    LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL).
    LP-284
  • HY-105019
    Melflufen
    Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
    Melflufen
  • HY-106024A
    Alagebrium bromide
    		Control
    Alagebrium bromide is an analog of Alagebrium Chloride (HY-106024B), a glucose cross-link blocker. Alagebrium Chloride disrupts glucose cross-links and may improve ventricular and arterial compliance. Alagebrium Chloride improves left ventricular diastolic filling and has the potential to inhibit diastolic heart failure (DHF).
    Alagebrium bromide
  • HY-W275553
    4-Decanol
    		Inhibitor
    4-Decanol is an antimutagenic compound, that can be isolated from mustard leaves. 4-Decanol inhibits mutagenic activities of Aflatoxin B1 (HY-N6615) and MNNG (HY-128612) in Salmonella typhimurium TA100.
    4-Decanol
  • HY-18987
    Duocarmycin MA
    Duocarmycin MA is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-agent resistant cell lines.
    Duocarmycin MA
  • HY-13567S1
    Bendamustine-d8
    Bendamustine-d8 is the deuterium labeled Bendamustine. Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
    Bendamustine-d<sub>8</sub>
  • HY-13593S1
    Chlorambucil-d8-1
    Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease.
    Chlorambucil-d<sub>8</sub>-1
  • HY-106435
    Cystemustine
    Cystemustine is a DNA inhibitor (a chloroethyl nitrosourea, CENU). Cystemustine can cause DNA cross-linking, thereby inhibiting the proliferation of tumor cells. Cystemustine can also exert cytotoxic effects by interfering with the cell cycle, inducing cell re-differentiation, and altering phospholipid metabolism. Cystemustine exhibits high anti-tumor activity and a relatively short plasma half-life in mice. Cystemustine can be used for the study of various malignant tumors, including melanoma, glioma, renal cancer, head and neck cancer, and colorectal cancer, etc.
    Cystemustine
  • HY-160057
    GMT 8 aptamer sodium
    GMT 8 aptamer sodium is a nucleic acid aptamer targeting different glioblastoma cell lines and exhibits high affinity. GMT 4 aptamer sodium also shows high binding affinity to the T lymphocyte cell line CCRF-CEM.
    GMT 8 aptamer sodium
  • HY-17420S1
    Cyclophosphamide-d8
    Cyclophosphamide-d8 is deuterium labeled Cyclophosphamide. Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.
    Cyclophosphamide-d<sub>8</sub>
  • HY-136327
    Phenylacetic acid mustard
    		Inhibitor
    Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil (HY-13593). Chlorambucil is an alkylating agent with antitumor activity.
    Phenylacetic acid mustard
  • HY-126782
    Lexitropsin 1
    Lexitropsin 1 is a DNA minor groove binder with a delta G degree of 65 kJ/mol at 303 K. Lexitropsin 1 has antiviral activity.
    Lexitropsin 1
  • HY-13732
    Prednimustine
    Prednimustine (Leo 1031;NSC 134087) is the ester formed from Prednisolone (HY-17463) and Chlorambucil (HY-13593). Prednimustine can be used for leukemias and lymphomas research.
    Prednimustine
  • HY-W717139
    N-Nitroso-N-methylurea-d5
    N-Nitroso-N-methylurea-d5 is the deuterium labeled N-Nitroso-N-methylurea (HY-34758). N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane.
    N-Nitroso-N-methylurea-d<sub>5</sub>
  • HY-W738282
    Bendamustine-d7 hydrochloride
    Bendamustine-d7 hydrochloride (SDX-105-d7) is the deuterium labeled Bendamustine hydrochloride (HY-B0077). 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.
    Bendamustine-d<sub>7</sub> hydrochloride
  • HY-111965
    PF-06647263
    PF-06647263 is an ADC targeting EFNA4, consisting of EFNA4 Antibody (HY-P991109), ADC toxin Calicheamicin (HY-19609) and a linker. PF-06647263 exhibits anti-tumor activity and induces significant tumor regression in TNBC xenografts.
    PF-06647263
Cat. No. Product Name / Synonyms Application Reactivity