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 (114):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101160
    SG2057
    98.67%
    SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.
    SG2057
  • 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-U00447
    PK11000
    ≥98.0%
    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-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-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-109146
    Imifoplatin
    Imifoplatin (PT-112) is a platinum-based agent belonging to the phosphaplatin family. Imifoplatin exhibits antineoplastic activity.
    Imifoplatin
  • HY-12456
    Duocarmycin SA
    ≥98.0%
    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-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-13747
    Semustine
    ≥98.0%
    Semustine is a DNA alkylator, binds to DNA, and acts as a cancer chemotherapeutic agent.
    Semustine
  • HY-17576
    Satraplatin
    99.82%
    Satraplatin is an alkylating agent, with potent antitumor effect.
    Satraplatin
  • 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-47820
    Tesirine intermediate-1
    99.41%
    Tesirine intermediate-1 is the intermediate of Tesirine (HY-128952). Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 (HY-101161), which has strong anticancer cell activity.
    Tesirine intermediate-1
  • HY-139813
    Phenanthriplatin
    Phenanthriplatin is a monovalent platinum(II)-based complex with a large cytotoxicity against cancer cells.
    Phenanthriplatin
  • 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-16405
    PR-104
    Inhibitor
    PR-104 is a selective hypoxia-activated DNA cross-linking agent and can be used for the research of multiple tumor xenograft models. PR-104, as a nitrogen mustard pre-proagent, is converted efficiently to the more lipophilic dinitrobenzamide mustards alcohol PR-104A.
    PR-104
  • HY-34477S1
    2-Iodoacetamide-d4
    99.90%
    2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide[1]. 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics[2][3].
    2-Iodoacetamide-d<sub>4</sub>
  • 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-16325A
    Miriplatin
    ≥98.0%
    Miriplatin (SM-11355) is a chemotherapy agent which belongs to the class of alkylating agents.
    Miriplatin
  • HY-129356A
    (S)-Seco-Duocarmycin SA
    ≥99.0%
    (S)-Seco-Duocarmycin SA is a DNA alkylator, cytotoxic to cancer cells, and acts as a ADC cytotoxin for antibody-drug conjugates.
    (S)-Seco-Duocarmycin SA
  • HY-129355
    Duocarmycin Analog
    Duocarmycin Analog is an analog of Duocarmycin, and used as an DNA alkylator and ADC cytotoxin.
    Duocarmycin Analog