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Topoisomerase I, Human

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15142
    Doxorubicin hydrochloride
    Maximum Cited Publications
    650 Publications Verification

    Hydroxydaunorubicin hydrochloride; ADR

    		 Topoisomerase ADC Payload AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Fluorescent Dye Infection Cancer
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride; ADR), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
    Doxorubicin hydrochloride
  • HY-16560
    Camptothecin
    65+ Cited Publications

    Campathecin; (S)-(+)-Camptothecin; CPT

    		 Topoisomerase ADC Payload MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Infection Cancer
    Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
    Camptothecin
  • HY-138298
    Trastuzumab deruxtecan (solution)
    5 Publications Verification

    T-DXd (solution); DS-8201 (solution); DS-8201a (solution)

    		 Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (T-DXd; DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
    Trastuzumab deruxtecan (solution)
  • HY-138298A
    Trastuzumab deruxtecan
    5 Publications Verification

    T-DXd; DS-8201; DS-8201a

    		 Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
    Trastuzumab deruxtecan
  • HY-141598
    Datopotamab deruxtecan (solution)
    2 Publications Verification

    DS-1062 (solution); Dato-DXd (solution)

    		 TROP2 Antibody-Drug Conjugates (ADCs) Topoisomerase Cancer
    Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
    Datopotamab deruxtecan (solution)
  • HY-128946
    CL2A-SN-38
    5 Publications Verification

    		 Drug-Linker Conjugates for ADC Inflammation/Immunology Cancer
    CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects .
    CL2A-SN-38
  • HY-15142R
    Doxorubicin hydrochloride (Standard)
    5 Publications Verification

    Hydroxydaunorubicin hydrochloride (Standard); ADR (Standard)

    		 Reference Standards Topoisomerase ADC Payload AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Fluorescent Dye Infection Cancer
    Doxorubicin hydrochloride (Standard) is the analytical standard of Doxorubicin hydrochloride. This product is intended for research and analytical applications. Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
    Doxorubicin hydrochloride (Standard)
  • HY-P99813
    Patritumab deruxtecan

    HER3-DXd; U3-1402

    		 Antibody-Drug Conjugates (ADCs) Cancer
    Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
    Patritumab deruxtecan
  • HY-164152A
    ADC Control Human IgG1-Deruxtecan (DAR 8)

    		Antibody-Drug Conjugates (ADCs) Topoisomerase Cancer
    ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
    ADC Control Human IgG1-Deruxtecan (DAR 8)
  • HY-15142A
    Doxorubicin

    Hydroxydaunorubicin

    		 ADC Payload Antibiotic Bacterial Topoisomerase AMPK HIV Autophagy Mitophagy Apoptosis HBV Fluorescent Dye Infection Cancer
    Doxorubicin (Hydroxydaunorubicin), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy .
    Doxorubicin
  • HY-164152
    ADC Control Human IgG1-Deruxtecan (DAR 4)

    		Antibody-Drug Conjugates (ADCs) Topoisomerase Cancer
    ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
    ADC Control Human IgG1-Deruxtecan (DAR 4)
  • HY-156617A
    (αR)-Cyclopropaneacetamide-Exatecan

    SHR169265

    		 ADC Payload Topoisomerase Cancer
    (αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer .
    (αR)-Cyclopropaneacetamide-Exatecan
  • HY-13631J
    (1R,9R)-Exatecan mesylate

    (1R,9R)-DX8951f

    		 Drug Derivative Topoisomerase Apoptosis Cancer
    (1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
    (1R,9R)-Exatecan mesylate
  • HY-13631I
    (1S,9R)-Exatecan mesylate

    (1S,9R)-DX8951f

    		 Drug Derivative Topoisomerase Apoptosis Cancer
    (1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia .
    The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
    (1S,9R)-Exatecan mesylate
  • HY-N3488
    Isodiospyrin

    		Topoisomerase Bacterial Fungal Infection Cancer
    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-125331
    DRF-1042

    		Topoisomerase ADC Payload Cancer
    DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
    DRF-1042
  • HY-126142
    Top1 inhibitor 1

    		Topoisomerase ADC Payload Cancer
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM .
    Top1 inhibitor 1
  • HY-16560S
    Camptothecin-d5

    Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5

    		 Isotope-Labeled Compounds Topoisomerase ADC Payload MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Infection Cancer
    Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
    Camptothecin-d5
  • HY-118899
    XR5944

    		Endogenous Metabolite Cancer
    XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
    XR5944
  • HY-W008874
    meso-Tetra(4-pyridyl)porphine

    		Topoisomerase Cancer
    meso-Tetra(4-pyridyl)porphine (Compound 10) is a porphyrin derivative. meso-Tetra(4-pyridyl)porphine is a weak inhibitor of human topoisomerase I (Top1) with an EC50 value greater than 50 µM. meso-Tetra(4-pyridyl)porphine can be used in tumor research .
    meso-Tetra(4-pyridyl)porphine
  • HY-P10765
    DTS-108

    		Peptide-Drug Conjugates (PDCs) Topoisomerase Cancer
    DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .
    DTS-108
  • HY-16560R
    Camptothecin (Standard)

    Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)

    		 Reference Standards Topoisomerase ADC Payload MicroRNA Influenza Virus Apoptosis Fungal Antibiotic Infection Cancer
    Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
    Camptothecin (Standard)
  • HY-121352
    Kibdelone C

    		Drug Derivative Cancer
    Kibdelone C is a hexacyclic tetrahydroxanthone natural product and anticancer agent with sub-nanomolar GI50 activity against human SR leukemia and SN12C renal carcinoma cell lines. Kibdelone C disrupts the actin cytoskeleton in human cancer cells, leading to cell contraction and actin stress fiber formation, without direct actin binding, actin polymerization effects, topoisomerase I/II inhibition, or DNA binding. Kibdelone C can be used for the research of leukemia, and renal cell carcinoma .
    Kibdelone C
  • HY-161385
    Topoisomerase I inhibitor 16

    		Topoisomerase Cancer
    Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
    Topoisomerase I inhibitor 16
  • HY-E71020
    Topoisomerase I, Human

    		Biochemical Assay Reagents Metabolic Disease
    Topoisomerase I, Human (EC 5.99.1.2) relaxes supercoiled DNA molecules. Topoisomerase I, Human (EC 5.99.1.2) initiates transient breakages and rejoins of phosphodiester bonds in superhelical turns of closed-circular DNA.
    Topoisomerase I, Human
  • HY-168739
    Topoisomerase I inhibitor 17

    		Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis Cancer
    Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
    Topoisomerase I inhibitor 17
  • HY-168632
    Topoisomerase I/II inhibitor 6

    		Topoisomerase Apoptosis Cancer
    Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3 .
    Topoisomerase I/II inhibitor 6
  • HY-N15319
    Eupolauridine

    Canangine

    		 Topoisomerase Fungal Infection
    Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases .
    Eupolauridine
  • HY-123143
    XR11576

    MLN576

    		 Topoisomerase Cancer
    XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
    XR11576
  • HY-156403
    AuM1Phe

    		Topoisomerase Cancer
    AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM .
    AuM1Phe
  • HY-178738
    GC-072

    		Antibiotic Bacterial Topoisomerase DNA/RNA Synthesis Infection
    GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis .
    GC-072
  • HY-162805
    iNOS/TopoI-IN-1

    		NO Synthase Topoisomerase Apoptosis NF-κB Inflammation/Immunology Cancer
    iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
    iNOS/TopoI-IN-1
  • HY-185370
    Doxorubicin liposome

    Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposome

    		 Liposome Topoisomerase Antibiotic Cancer
    Doxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
    Doxorubicin liposome
  • HY-E70900
    Topoisomerase II β, Human

    		Topoisomerase Metabolic Disease
    Topoisomerase II β, Human (EC 5.99.1.3) is a nuclear enzyme that play essential roles in DNA replication, transcription, chromosome segregation, and recombination. All cells have two major forms of topoisomerases: type I, which makes single-stranded cuts in DNA, and type II enzymes, which cut and pass double-stranded DNA.
    Topoisomerase II β, Human
  • HY-E70901
    Topoisomerase II α, Human

    		Topoisomerase Metabolic Disease
    Topoisomerase II α, Human (EC 5.99.1.3) is a nuclear enzyme that play essential roles in DNA replication, transcription, chromosome segregation, and recombination. All cells have two major forms of topoisomerases: type I, which makes single-stranded cuts in DNA, and type II enzymes, which cut and pass double-stranded DNA.
    Topoisomerase II α, Human
  • HY-N19312
    Diospyrin

    		Apoptosis Glutathione S-transferase Topoisomerase Cancer
    Diospyrin is a dinaphthoquinone anticancer agent with pro-apoptotic (apoptosis) activity, glutathione S-transferase (Glutathione S-transferase) inhibitory activity, and topoisomerase (Topoisomerase) I inhibitory activity. Diospyrin is present in the heartwood of various Diospyros plants and can be used for research on Ehrlich ascites carcinoma, acute myeloid leukemia, chronic myeloid leukemia, mammary adenocarcinoma, cervical epithelial carcinoma, malignant cutaneous melanoma, laryngeal epidermoid carcinoma, human osteosarcoma, and human lymphoblastic carcinoma .
    Diospyrin
  • HY-P992130
    Rolditamig

    TQB2102 Antibody

    		 ADC Antibody EGFR Cancer
    Rolditamig (TQB2102 Antibody) is a recombinant humanized anti-human epidermal growth factor receptor 2 (HER2) antibody. Rolditamig can be conjugated with an enzyme-cleavable linker and a topoisomerase I inhibitor to form the ADC TQB2102. Rolditamig is applicable to research on solid tumors such as HER2-positive breast cancer .
    Rolditamig

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