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-Y1155S
    Hexamethylphosphoramide-d18
    Hexamethylphosphoramide-d18 is the deuterium labeled Hexamethylphosphoramide (HY-Y1155). Hexamethylphosphoramide is an orally active polar aprotic solvent, flame retardant additive, and carcinogen. Hexamethylphosphoramide undergoes cytochrome P-450-mediated N-demethylation to Formaldehyde. Hexamethylphosphoramide induces DNA-protein crosslinks. Hexamethylphosphoramide has been linked to nasal tumors (squamous cell carcinoma, adenoid squamous cell carcinoma), squamous metaplasia, rhinitis, tracheitis, and reversible and irreversible infertility.
    Hexamethylphosphoramide-d<sub>18</sub>
  • 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-126929
    Trioxacarcin B
    Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma.
    Trioxacarcin B
  • HY-133240
    trans-AzoTAB
    trans-AzoTAB is a photoresponsive potassium/sodium/calcium channel modulator and DNA-binding agent. trans-AzoTAB undergoes trans-cis isomerization driven by light, with variable polarity and DNA affinity. trans-AzoTAB also enhances voltage-gated potassium currents and inhibits sodium and calcium currents in cardiomyocytes, thereby reducing spontaneous electrical activity and excitation conduction velocity. In addition, trans-AzoTAB induces compaction and frozen conformation of λ-phage DNA, and non-sequence-dependently inhibits transcription and translation processes in the dark; its activity can be reversed and restored by visible light after activation with ultraviolet irradiation. trans-AzoTAB can serve as a probe for two-photon optical regulation of myocardial excitability, and is used to construct photoresponsive interfacial polymer structures.
    trans-AzoTAB
  • HY-183291
    Antibacterial agent 343
    Antibacterial agent 343 (Compound 47) is an Antibacterial agent. Antibacterial agent 343 binds to the allosteric site of PBP2a to open its active site. Antibacterial agent 343 disrupts bacterial cell membranes, leading to protein leakage. Antibacterial agent 343 interacts with DNA and inhibits replication and transcription. Antibacterial agent 343 induces ROS accumulation. Antibacterial agent 343 exhibits antibacterial activity against MRSA, Staphylococcus aureus, and Enterococcus faecalis. Antibacterial agent 343 can be used for the research of methicillin-resistant Staphylococcus aureus infections.
    Antibacterial agent 343
  • HY-118823
    Amonafide L-malate
    Amonafide L-malate is a topoisomerase II inhibitor and DNA intercalator that induces Apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide L-malate
  • HY-18774
    Cycloplatam
    Cycloplatam is a DNA crosslinking agent. Cycloplatam inhibits tumor cell DNA replication and transcription. Cycloplatam is promising for research of ovarian cancer, lung cancer, and other solid tumors.
    Cycloplatam
  • HY-19257
    Triplatin tetranitrate
    Triplatin tetranitrate is a novel trinuclear platinum complex. Triplatin tetranitrate blocks G2/M phase. Triplatin tetranitrate can covalently bind to the DNA bases. Triplatin tetranitrate exhibits significant antitumor effects against neuroblastoma.
    Triplatin tetranitrate
  • HY-106091B
    Losoxantrone hydrochloride
    Losoxantrone hydrochloride (CI 941 hydrochloride) is a DNA-binding agent. Losoxantrone hydrochloride has broad-spectrum antitumour activity. Losoxantrone hydrochloride induces dose-dependent leukopenia.
    Losoxantrone hydrochloride
  • 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-W338604
    Prospidium dichloride
    Prospidium dichloride is a cationic cytostatic agent and anticancer agent.
    Prospidium dichloride
  • HY-119044
    KW-2149
    KW-2149 (KT-6149) is a Mitomycin C (HY-13316) analogue activated by serum. KW-2149 can interact with DNA. KW-2149 exhibits antitumor activity. KW-2149 has pulmonary toxicity KW-2149 can be used for the research of cancer, such as leukemia.
    KW-2149
  • 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-106091
    Losoxantrone
    Losoxantrone (CI 941) is a DNA-binding agent. Losoxantrone has broad-spectrum antitumour activity. Losoxantrone induces dose-dependent leukopenia.
    Losoxantrone
  • 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
Cat. No. Product Name / Synonyms Application Reactivity