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-148424
    PBD dimer-2
    		98.03%
    PBD dimer-2 (compound 2c) is a C8-linked pyrrolobenzodiazepine dimer. PBD dimer-2 can span an extra base pair and cross-link the 5′-Pu-GA(T/A)TC-Py sequence. PBD dimer-2 can be used as a payload for antibody–agent conjugates (ADCs), and it can be used for the research of cancer.
    PBD dimer-2
  • HY-13543
    Tretazicar
    		99.65%
    Tretazicar (CB 1954), an antitumor proagent, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involves the reduction of its 4-nitro group to a 4-hydroxylamine by the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1).
    Tretazicar
  • HY-W015854
    Ethyl methanesulfonate
    		99.96%
    Ethyl methanesulfonate is an orally active biochemical agent. Ethyl methanesulfonate induces Apoptosis. Ethyl methanesulfonate acts on DNA, alkylating it and causing changes in DNA structure, which in turn triggers a series of biological effects such as mutation and cell death. Ethyl methanesulfonate induces kidney and nervous system tumors. Ethyl methanesulfonate is widely used in the field of genetic toxicology research and is often used to induce gene mutations in organisms to study gene function, the mechanism of genetic diseases, and the effects of environmental mutagenic factors, etc.
    Ethyl methanesulfonate
  • 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. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
    PIP-199
  • HY-124573
    OBI-3424
    		99.23%
    OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.
    OBI-3424
  • HY-12456
    Duocarmycin SA
    		99.55%
    Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
    Duocarmycin SA
  • HY-125098
    Illudin S
    		98.01%
    Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells.
    Illudin S
  • HY-109146
    Imifoplatin
    Imifoplatin (PT-112) is a platinum-based active molecule and a member of the phosphaplatins family. Imifoplatin can induce Apoptosis and exhibits antitumor activity.
    Imifoplatin
  • HY-16503
    Treosulfan
    		≥98.0%
    Treosulfan (NSC 39069) is a bifunctional alkylating agent with activity in ovarian cancer and other solid tumor types.
    Treosulfan
  • HY-13703A
    Nimustine hydrochloride
    		98.22%
    Nimustine hydrochloride (ACNU) is a DNA cross-linking and DNA alkylating agent, which induces DNA replication blocking lesions and DNA double-strand breaks and inhibits DNA synthesis, commonly used in chemotherapy for glioblastomas.
    Nimustine hydrochloride
  • HY-111397
    Bizelesin
    Bizelesin (NSC 615291; U-77779) is an AT-specific DNA alkylating agent that can generate DNA interstrand crosslinks, effectively inhibit DNA replication, and has potential anticancer activity.
    Bizelesin
  • HY-17576
    Satraplatin
    		99.79%
    Satraplatin is an alkylating agent, with potent antitumor effect.
    Satraplatin
  • HY-14429
    (-)-Irofulven
    		98.86%
    (-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity.
    (-)-Irofulven
  • HY-B0733
    Fotemustine
    Fotemustine is a DNA-alkylating agent, with antitumor activity.
    Fotemustine
  • HY-16398
    Pipobroman
    		99.81%
    Pipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al.
    Pipobroman
  • HY-B0245S
    Busulfan-d8
    		≥99.0%
    Busulfan-d8 is a deuterium labeled Busulfan. Busulfan is a potent alkylating antineoplastic agent. Busulfan causes DNA damage by cross-linking DNAs and DNA and proteins. Busulfan inhibits thioredoxin reductase. Busulfan induces apoptosis. Busulfan is an immunosuppressive and myeloablative chemotherapeutic agent[1][2][3].
    Busulfan-d<sub>8</sub>
  • HY-17364S
    Temozolomide-d3
    		99.80%
    Temozolomide-d3 is the deuterium labeled Temozolomide. 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[1][2].
    Temozolomide-d<sub>3</sub>
  • HY-128873
    Duocarmycin GA
    		99.00%
    Duocarmycin GA is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-agent resistant cell lines.
    Duocarmycin GA
  • HY-U00447
    PK11000
    		99.56%
    PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities.
    PK11000
  • HY-139813
    Phenanthriplatin
    Phenanthriplatin is a monovalent platinum(II)-based complex with a large cytotoxicity against cancer cells.
    Phenanthriplatin
Cat. No. Product Name / Synonyms Application Reactivity