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-43564
    Exatecan Intermediate 5
    		Inhibitor 99.98%
    Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
    Exatecan Intermediate 5
  • HY-137466
    ARN-21934
    		Inhibitor 98.08%
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
    ARN-21934
  • HY-148380A
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
    		Inhibitor 98.44%
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA is a agent-linker conjugate for ADC, composed of degradable linker Mal-PEG8-Phe-Lys-PAB and toxin molecule Exatecan (HY-13631).
    Mal-PEG8-Phe-Lys-PAB-Exatecan TFA
  • HY-106031
    F-14512
    F-14512 is a targeted cytotoxic compound that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 combines an epipodophyllotoxin core that targets topoisomerase II with a spermine group that acts as a cell delivery vehicle, with improved selectivity for tumor cells. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and demonstrates high potency in multiple human cell lines (median IC50=0.18 μM). In the MX1 breast tumor xenograft model, F-14512 exhibits potent antitumor activity.
    F-14512
  • 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-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-160015
    CB07-Exatecan
    		Inhibitor 98.97%
    CB07-Exatecan is an ADC drug-Linker conjugate that can be used for the synthesis of ADCs. ADC conjugated with CB07-Exatecan and trastuzumab inhibits the growth of HER2-positive cancer cells. CB07-Exatecan can be used in cancer research.
    CB07-Exatecan
  • HY-160409
    TopBP1-IN-1
    		Inhibitor 98.35%
    TopBP1-IN-1 is a TopBP1 inhibitor. TopBP1-IN-1 has a synergistic effect with PARP inhibitors. TopBP1-IN-1 has antitumor activity .
    TopBP1-IN-1
  • 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-153069
    GGFG-PAB-Exatecan
    		Inhibitor 99.71%
    GGFG-PAB-Exatecan consists of an ADC toxin Exatecan (HY-13631) and a linker GGFG-PAB, and can be used as a drug-linker conjugate for the synthesis of ADC molecules.
    GGFG-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-B0330B
    Levofloxacin hydrochloride
    		Inhibitor 98.0%
    Levofloxacin hydrochloride is an orally active antibiotic. Levofloxacin inhibits DNA gyrase and topoisomerase IV activity, inducing Apoptosis. Levofloxacin hydrochloride has antibacterial activity against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride exhibits anticancer activity against lung cancer. Levofloxacin hydrochloride has anti-acnegenic, anxiogenic, and analgesic effects. Levofloxacin hydrochloride shortens sleep duration in mice. Levofloxacin hydrochloride can be used in the research of infectious diseases (such as tuberculosis, chronic periodontitis, bacterial infections associated with stable COPD, and BK viremia) and lung cancer.
    Levofloxacin hydrochloride
  • 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-N0114A
    (±)-Evodiamine
    		Inhibitor 99.74%
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis.
    (±)-Evodiamine
  • HY-153600
    GGFG-amide-glycol-amide-Exatecan
    		Inhibitor 98.73%
    GGFG-amide-glycol-amide-Exatecan (Intermediate 2) is an Exatecan (HY-13631) derivative and can be used in the synthesis of antibody-drug conjugates (ADCs).
    GGFG-amide-glycol-amide-Exatecan
  • HY-N6011
    9-Methoxycamptothecin
    		Inhibitor 99.13%
    9-Methoxycamptothecin (MCPT), isolated from Camptotheca acuminata, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
    9-Methoxycamptothecin
  • 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-17460A
    Garenoxacin Mesylate hydrate
    		Inhibitor 99.78%
    Garenoxacin (BMS284756) Mesylate hydrate is an orally active quinolone antibiotic and has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes, and fastidious organisms.
    Garenoxacin Mesylate hydrate
  • 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-N8248
    Eleutherin
    		99.22%
    Eleutherin is a type of naphthoquinone derivative with the protective effect against the injury ofhuman umbilical vein endothelial cells (HUVECs), which can be isolated from the edible bulbs of Eleutherine americana (Hong-Cong).
    Eleutherin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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