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-16562S1
    Irinotecan-d10 hydrochloride
    		Inhibitor 99.76%
    Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan-d<sub>10</sub> hydrochloride
  • 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-153031
    Val-Cit-PAB-Exatecan
    		Inhibitor 99.79%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan
  • HY-N0311
    Emodin-8-glucoside
    		Inhibitor 99.35%
    Emodin-8-glucoside is an anthraquinone derivative that can be isolated from Aloe vera. Emodin-8-glucoside is the inhibitor for MAPK with an inhibition constant of 430.14 pM. Emodin-8-glucoside exhibits moderate inhibitory activity against rat lens aldose reductase (ALAR) and topoisomerases II with IC50s of 14.4 μM and 66 μM. Emodin-8-glucoside exhibits antioxidant, anti-inflammatory and anti-fibrotic activities. Emodin-8-glucoside can cross the blood brain barrier.
    Emodin-8-glucoside
  • HY-101647
    Intoplicine
    		Inhibitor 98.36%
    Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
    Intoplicine
  • 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-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-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-B0330R
    Levofloxacin (Standard)
    		Inhibitor 99.96%
    Levofloxacin (Standard) is the analytical standard of Levofloxacin. This product is intended for research and analytical applications. Levofloxacin ((-)-Ofloxacin) is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin inhibits the DNA gyrase and topoisomerase IV. Levofloxacin can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin shows anti-orthopoxvirus activity.
    Levofloxacin (Standard)
  • 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-10581A
    Gatifloxacin hydrochloride
    		Inhibitor 99.94%
    Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
    Gatifloxacin hydrochloride
  • 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-13566AS
    Belotecan-d7 hydrochloride
    		Inhibitor 99.90%
    Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.
    Belotecan-d<sub>7</sub> hydrochloride
  • HY-156617A
    (αR)-Cyclopropaneacetamide-Exatecan
    		Inhibitor 99.75%
    (αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, is a cytotoxic agent. (αR)-Cyclopropaneacetamide-Exatecan inhibits U87MG and SK-BR-3 cells proliferation, with IC50s of 8.11 and 2.31 μM.
    (αR)-Cyclopropaneacetamide-Exatecan
  • 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
  • HY-N6714
    Alternariol
    		Inhibitor 99.67%
    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-N0872
    Isosteviol
    		Inhibitor ≥98.0%
    Isosteviol ((-)-Isosteviol) is a derivative of Stevioside through acid catalyzed hydrolysis of Stevioside. Isosteviol inhibits DNA polymerase and DNA topoisomerase and has antibacterial, anticancer and anti-tuberculosis effects.
    Isosteviol
  • HY-153797
    Dox-btn2
    		Inhibitor
    Dox-btn2 is a biotin labeled Doxorubicin (HY-15142A), with a biotin label at the point of conjugation to doxorubicin at 3'-NH2. Dox-btn2 can be used for cell imaging. While Doxorubicin is mainly accumulated in the nucleus, while Dox-btn2 is mainly located in the cytoplasm.
    Dox-btn2
  • HY-17028
    Besifloxacin Hydrochloride
    		Inhibitor 98.11%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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