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Results for "

human DNA Topoisomerase I

" in MedChemExpress (MCE) Product Catalog:

32

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4

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1

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Targets Recommended:
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-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-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-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-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-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-164729
    FZ-AD005

    		Antibody-Drug Conjugates (ADCs) Topoisomerase Apoptosis Cancer
    FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
    FZ-AD005
  • 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-100777
    DACA

    		Topoisomerase Neurological Disease Cancer
    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-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-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-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-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-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-100777R
    DACA (Standard)

    		Topoisomerase Reference Standards Cancer
    DACA (Standard) is the analytical standard of DACA (HY-100777). This product is intended for research and analytical applications. DACA (XR 5000) is a blood-brain barrier-penetrating topoisomerase I and II inhibitor. DACA can be used in the research of colorectal cancer, leukemia and lung cancer .
    DACA (Standard)
  • 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-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-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-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-N8250
    cis-THSG

    		Topoisomerase PEPCK Metabolic Disease
    cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus .
    cis-THSG
  • HY-182816
    Topoisomerase I-IN-22

    		Topoisomerase DNA/RNA Synthesis Bacterial Infection
    Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection .
    Topoisomerase I-IN-22
  • HY-182748
    NL-26

    		Topoisomerase DNA/RNA Synthesis Apoptosis Cancer
    NL-26 is a Topoisomerase I inhibitor. NL-26 stabilizes the covalent Topoisomerase I (Topo I)-DNA complex, prevents DNA religation and triggers the DNA damage response. NL-26 induces G2/M cell cycle arrest and apoptosis in cancer cells. NL-26 can be used for the research of colorectal cancer .
    NL-26

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