2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.

Topoisomerase Isoform Specific Products:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13744
    Rubitecan
    		Inhibitor 99.23%
    Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
    Rubitecan
  • HY-N0354
    Anthraquinone
    		Inhibitor 99.12%
    Anthraquinone is used as a precursor for dye formation and agrochemicals, existing in different organisms, such as bacteria, fungi, plants, and some animals. Anthraquinone has biological activities: anticancer, antiinflammatory, diuretic, antiarthritic, antifungal, antibacterial, antimalarial and antioxidant. Anthraquinone also plays an important role in the primary metabolism of plants by acting on the electron transport chain through the inhibition of energy transfer in the photosynthetic process. Anthraquinone can intercalates into DNA and inhibits the topoisomerase II (topo II) enzyme, resulting in cell death via Apoptosis.
    Anthraquinone
  • HY-N6714
    Alternariol
    		Inhibitor 99.88%
    Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol
  • HY-143692
    SQDG
    		Inhibitor 99.0%
    SQDG inhibits topoisomerase I and P-selectin receptor, exhibits anti-inflammatory, antiviral and antitumor activities. SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations.
    SQDG
  • HY-N3488
    Isodiospyrin
    		Inhibitor 99.77%
    Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities.
    Isodiospyrin
  • HY-156748
    MC-PEG2-VA-PAB-Exatecan
    		Inhibitor 99.61%
    MC-PEG2-VA-PAB-Exatecan (Compound DL-18) is a Drug-Linker Conjugates for ADC. MC-PEG2-VA-PAB-Exatecan consists of Exatecan (HY-13631) and a linker. MC-PEG2-VA-PAB-Exatecan can be used for synthesis of ADCs.
    MC-PEG2-VA-PAB-Exatecan
  • HY-B0063
    Gimatecan
    		Inhibitor 99.28%
    Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
    Gimatecan
  • HY-158109
    M3554
    		Inhibitor 99.39%
    M3554 is an anti-GD2 antibody-drug conjugate (ADC) based on the humanized anti-GD2 antibody. M3554 consists of the humanized monoclonal antibody hu14.18 (K322A) (HY-P991040) linked to a topoisomerase 1 inhibitor Exatecan (HY-13631) via a cleavable β-glucuronide linker. M3554 can be used for the study of neuroblastoma, osteosarcoma or glioma.
    M3554
  • HY-106662
    Chloroquinoxaline sulfonamide
    		Inhibitor 99.06%
    Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle. Antitumor activity.
    Chloroquinoxaline sulfonamide
  • HY-159783
    Mal-Exatecan
    		Inhibitor 99.39%
    Mal-Exatecan is a Mal (Maleimide) modified Exatecan (HY-13631), a DNA topoisomerase I (topoisomerase I) inhibitor.
    Mal-Exatecan
  • HY-171580
    Mc-PEG4-Val-Ala-PAB-Exatecan
    		Inhibitor 99.65%
    Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631).
    Mc-PEG4-Val-Ala-PAB-Exatecan
  • HY-U00248
    LMP744
    		Inhibitor 98.85%
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744
  • HY-13704R
    SN-38 (Standard)
    		Inhibitor
    SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38 (Standard)
  • HY-13758A
    TAS-103 dihydrochloride
    		Inhibitor 98.45%
    TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
    TAS-103 dihydrochloride
  • HY-B1050
    Gemifloxacin mesylate
    		Inhibitor 99.76%
    Gemifloxacin mesylate (SB-265805S; LB-20304a) is an orally active broad-spectrum quinolone antibacterial antibiotic. Gemifloxacin mesylate inhibits DNA synthesis by inhibiting DNA gyrase and Topoisomerase IV activities. Gemifloxacin mesylate has potent antibacterial activities against gram-positive bacteria in vitro efficacy study, particularly Streptococci and Staphylococci. Gemifloxacin mesylate has been used in the research of respiratory tract infections.
    Gemifloxacin mesylate
  • HY-100875A
    Bisantrene dihydrochloride
    		Inhibitor 98.85%
    Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1.
    Bisantrene dihydrochloride
  • HY-U00248A
    LMP744 hydrochloride
    		Inhibitor 99.08%
    LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744 hydrochloride
  • HY-17028
    Besifloxacin Hydrochloride
    		Inhibitor 98.49%
    Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research.
    Besifloxacin Hydrochloride
  • HY-400770
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
    		Inhibitor
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1 (compound 19-2) is an intermediate for the synthesis of MC-GGFG-AM-(10Me-11F-Camptothecin) (HY-153360). Modifying groups can be added group. MC-GGFG-AM-(10Me-11F-Camptothecin) is a drug-linker conjugate used in the synthesis of ADCs.
    MC-GGFG-AM-(10Me-11F-Camptothecin) intermediate-1
  • HY-157813
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
    		Inhibitor 98.27%
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan is a drug-linker conjugates for ADC, consiting of a cleavable linker and Exatecan (HY-13631). 2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan can be linked to anti-Her3 antibody.
    2-MSP-5-HA-GGFG-NH-CH2-O-CH2-CO-Exatecan
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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