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

DNA Alkylator/Crosslinker

DNA Alkylator/Crosslinker

Related Products

PDF 0.35 MB

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-129356
    Seco-Duocarmycin SA
    Seco-Duocarmycin SA is a DNA alkylator. Seco-Duocarmycin SA is an antitumor antibiotic (IC50 = 10 pM). Seco-Duocarmycin SA can induce a concentration-dependent increase in apoptotic cell death. Seco-Duocarmycin SA can lead to significant cell cycle arrest in S and G2/M phases. Seco-Duocarmycin SA acts as an ADC cytotoxin for antibody-drug conjugates.
    Seco-Duocarmycin SA
  • HY-144335
    DNA crosslinker 2 dihydrochloride
    DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer.
    DNA crosslinker 2 dihydrochloride
  • HY-164303
    Val-Cit-PAB-DEA-Duo-DM
    		Inhibitor
    Val-Cit-PAB-DEA-Duo-DM is a drug-linker conjugate, which consists of the linker Val-Cit-PAB, the spacer DEA and the ADC toxin Duocarmycin DM (Duo-DM) (HY-130978). Val-Cit-PAB-DEA-Duo-DM can be used for the synthesis of ADC molecule.
    Val-Cit-PAB-DEA-Duo-DM
  • HY-139621
    Colibactin 742
    Colibactin 742 is a covalently binding DNA-damaging agent targeting DNA, with an IC50 of 5.2 μM against human cervical cancer cells (HeLa). Colibactin 742 covalently binds to DNA, forming interstrand crosslinks (ICLs), activating the Fanconi anemia DNA repair pathway, inducing γH2AX and FANCD2 foci formation and cell cycle arrest, while exacerbating mismatch repair deficiency (MMRd)-related mutations. Colibactin 742 can mimic the genotoxicity of natural Colibactin while avoiding its instability, and is mainly used in colorectal cancer (CRC) related research, including microbial tumorigenesis mechanisms, DNA damage repair pathways, and mutation signature analysis.
    Colibactin 742
  • HY-105890
    Spiroplatin
    Spiroplatin is a Cisplatin (HY-17394) congener and has antitumor activity.
    Spiroplatin
  • HY-176807
    DBCO-HS-PEG2-VA-PABC-SG3199
    		Inhibitor
    DBCO-HS-PEG2-VA-PABC-SG3199 is a drug-linker conjugate for ADC. DBCO-HS-PEG2-VA-PABC-SG3199 consists of a SG3199 (HY-101161) based DNA small channel crosslinker and cleavable linker. DBCO-HS-PEG2-VA-PABC-SG3199 can be used for synthesis of ADCs.
    DBCO-HS-PEG2-VA-PABC-SG3199
  • HY-13733R
    Procarbazine Hydrochloride (Standard)
    Procarbazine (Hydrochloride) (Standard) is the analytical standard of Procarbazine (Hydrochloride). This product is intended for research and analytical applications. Procarbazine Hydrochloride is an orally active alkylating agent, with anticancer activity. Procarbazine Hydrochloride can be used in Hodgkin's disease research.
    Procarbazine Hydrochloride (Standard)
  • HY-B0077S1
    Bendamustine-d8 hydrochloride
    Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). 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>8</sub> hydrochloride
  • HY-119228
    SN-28049
    SN-28049 is a new DNA-binding topoisomerase II-directed antitumor agent. SN-28049 activates the p53 pathway. SN-28049 exhibits anticancer activity against colorectal cancer.
    SN-28049
  • HY-106768
    Trimelamol
    Trimelamol (CB10-375; NSC283162) is a highly efficient acid-catalyzed DNA interstrand crosslinker with low neurotoxicity due to its limited BBB penetration. Trimelamol exhibits anti-tumor activity and overcomes platinum resistance. Trimelamol is investigated for lung and ovarian cancer research[1][2][3][4][5].
    Trimelamol
  • HY-17419A
    (R)-Ifosfamide
    (R)-Ifosfamide is a chemotherapeutic agent primarily used in the treatment of aggressive tumors such as rhabdomyosarcoma, exhibiting alkylating activity that interferes with DNA replication. (R)-Ifosfamide is an isomeric derivative of the DNA alkylating agent Ifosfamide (HY-17419).
    (R)-Ifosfamide
  • HY-179392
    Sunitinib-platinum(IV) prodrug-1
    		Inducer
    Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma.
    Sunitinib-platinum(IV) prodrug-1
  • HY-133590
    Heliotrine N-oxide
    Heliotrine N-oxide is the corresponding PA (pyrrolizidine alkaloid) N-oxide of Heliotrine (HY-126128). Heliotrine N-oxide leads to the formation of pyrrolic DNA adducts and potential initiation of PA-induced liver tumors in vivo.
    Heliotrine N-oxide
  • HY-N18080
    Parthenin
    Parthenin is a pseudoguaianolide-type sesquiterpene lactone present in Parthenium hysterophorus L. Parthenin induces chromosomal aberrations, mainly chromatid breaks, in human peripheral blood lymphocytes. Parthenin exhibits toxicity against Salmonella typhimurium and Escherichia coli strains, with reduced toxicity in the presence of a metabolic activation system (S9). Parthenin acts as an antifeedant against the 6th instar larvae of the tobacco cutworm (Spodoptera litura). Parthenin shows insecticidal activity against adult cowpea weevils (Callosobruchus maculatus). Parthenin inhibits seed germination and seedling growth of sicklepod (Cassia tora). Parthenin possesses nematicidal activity against the 2nd instar larvae of the southern root-knot nematode (Meloidogyne incognita). Parthenin serves as a research agent for studies related to cancer, malaria, amoebiasis, inflammatory diseases, and bacterial infections.
    Parthenin
  • HY-171685
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA
    		Inducer
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated with the linker MC-Vc-PAB-DMEA-PEG2 and the DNA alkylator Duocarmycin SA (HY-12456). Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA can be used in cancer research.
    Anti-CCL2 (Carlumab)-MC-Vc-PAB-DMEA-PEG2-Duocarmycin SA
  • HY-148091
    Duocarmycin analog-2
    Duocarmycin analog-2 is a potent DNA alkylating agent. Duocarmycin analog-2 can be used of synthetic immunoconjugate. Duocarmycin analog-2 has antitumor activity.
    Duocarmycin analog-2
  • HY-106588
    Heptaplatin
    Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles.
    Heptaplatin
  • HY-185488
    seco-CBI dimer
    seco-CBI dimer is a DNA alkylating agent and a prodrug of Duocarmycin, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). seco-CBI dimer binds to the minor groove of A-T-rich regions in DNA, alkylates the N3 position of adenine residues, and induces DNA strand breaks. seco-CBI dimer can be used in the research of non-Hodgkin's lymphoma.
    seco-CBI dimer
  • HY-185492
    MC-cBu-Cit-seco-CBI dimer
    MC-cBu-Cit-seco-CBI dimer (Compound 10) is a conjugate of an ADC drug toxin molecule and a linker, which consists of a DNA alkylating agent connected to a reactive maleimide via a protease-cleavable peptidomimetic linker.
    MC-cBu-Cit-seco-CBI dimer
  • HY-13567A
    Bendamustine hydrochloride hydrate
    Bendamustine hydrochloride hydrate (SDX-105 hydrate), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride hydrate activates DNA-damage stress response and apoptosis. Bendamustine hydrochloride hydrate has potent alkylating, anticancer and antimetabolite properties.
    Bendamustine hydrochloride hydrate
Cat. No. Product Name / Synonyms Application Reactivity