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-100777
    DACA
    		Inhibitor 98.89%
    DACA (XR 5000) is a potential and blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer.
    DACA
  • 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-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-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-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-N3488
    Isodiospyrin
    		Inhibitor 99.72%
    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-173639
    AZD0516
    		Inhibitor 99.15%
    AZD0516 is a first-in-class antibody-drug conjugate (ADC) targeting six-transmembrane epithelial antigen of the prostate-2 (STEAP2). The anti-STEAP2 monoclonal antibody (mAb) is conjugated via interchain cysteines to a maleimide-reactive, β-glucuronidase-cleavable linker (HY-173635) bearing the topoisomerase 1 inhibitor, Exatecan (HY-13631). AZD0516 can be used for the study of prostate cancer.
    AZD0516
  • 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-164835
    VcMMAE-Deruxtecan
    		Inhibitor 98.10%
    VcMMAE-Deruxtecan (VcMMAE-(PAB-GGFG-AMAA)Exatecan; SMP-54418) is a drug-linker conjugate for ADC, composed of linker-payload molecule conjugate VcMMAE (HY-15575) and linker-payload molecule conjugate Deruxtecan (PAB-GGFG-AMAA)Exatecan) (HY-13631E). VcMMAE-Deruxtecan can be used in the synthesis of ADCs.
    VcMMAE-Deruxtecan
  • 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-13721
    Phenoxodiol
    		Inhibitor 99.89%
    Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.
    Phenoxodiol
  • HY-153278
    Q901
    		98.38%
    Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer.
    Q901
  • 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
  • HY-12930
    SPR719
    		Inhibitor 99.39%
    SPR719 (VXc-486) is an orally active gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively. SPR719 is promising for research of lung disease caused by non-tuberculous mycobacteria (NTM).
    SPR719
  • HY-164143
    T638
    		Inhibitor 98.61%
    T638 is a topoisomerase II (TOP2) inhibitor. T638 inhibits TOP2A activity with a IC50 of 0.7 uM. T638 strongly inhibits cancer cell growth.
    T638
  • HY-U00248
    LMP744
    		Inhibitor 98.33%
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
    LMP744
  • HY-10534
    Voreloxin
    		Inhibitor 99.85%
    Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin
  • 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-160005
    LMP517
    		Inhibitor 99.58%
    LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer.
    LMP517
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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