Topoisomerase
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
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Topoisomerase Inhibitors
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Topoisomerase Agonists
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Topoisomerase Modulator
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Topoisomerase Inducer
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Topoisomerase Degraders
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Topoisomerase Controls
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Topoisomerase Ligands
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Topoisomerase Proteins
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DNA topoisomerase II Proteins
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Topoisomerase Produits associés (812)
Produits associés (812)
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Protéines Recombinantes (1)
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Anticorps (4)
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Topoisomerase Isoform Comparison
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Doxorubicin hydrochloride
0 ImagesSynonyms: Hydroxydaunorubicin hydrochloride; ADRDoxorubicin 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.
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Etoposide
0 ImagesSynonyms: VP-16; VP-16-213Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
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DXd
0 ImagesSynonyms: Exatecan derivative for ADCDXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
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SN-38
0 ImagesSynonyms: 7-Ethyl-10-hydroxycamptothecinSN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. 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).
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Exatecan mesylate
0 ImagesSynonyms: DX8951fExatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
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Q901 TFA
0 ImagesCat. No.: HY-153278ASynonyms: CDK7-IN-21 TFAQ901 (CDK7-IN-21) TFA is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 TFA disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 TFA can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 TFA can be used for the research of cancer, such as colon cancer and lung cancer.
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Mocertatug rezetecan
0 ImagesCat. No.: HY-185280CAS No.: 3042848-25-6Synonyms: HS-20089; GSK5733584Mocertatug rezetecan (HS-20089) is an antibody-drug conjugate (ADC) targeting B7-H4, composed of Mocertatug (HY-P991703) and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (HY-148668). Mocertatug rezetecan delivers a TOPO1 inhibitor payload. It binds to B7-H4-expressing tumor cells, triggers ADC internalization, and induces S-phase cell cycle arrest, cytotoxicity, and bystander killing effect. Mocertatug rezetecan exhibits dose-dependent tumor growth inhibition in breast cancer and endometrial cancer CDX models. It can be used in research related to platinum-resistant ovarian cancer, breast cancer, endometrial cancer, cholangiocarcinoma, and cervical cancer.
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Doxorubicin liposome
0 ImagesCat. No.: HY-185370Synonyms: Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposomeDoxorubicin 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.
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Exatecan
0 ImagesSynonyms: DX-8951Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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Irinotecan
0 ImagesSynonyms: (+)-Irinotecan; CPT-11; VAL-413free baseIrinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
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Camptothecin
0 ImagesSynonyms: Campathecin; (S)-(+)-Camptothecin; CPTCamptothecin (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.
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Datopotamab deruxtecan (solution)
0 ImagesSynonyms: DS-1062 (solution); Dato-DXd (solution)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.
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Berberine chloride
0 ImagesBerberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
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Topotecan hydrochloride
0 ImagesSynonyms: SKF 104864A hydrochloride; NSC 609669 hydrochlorideTopotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
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Mitoxantrone
0 ImagesSynonyms: Mitozantrone; NSC 301739Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
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Exatecan-d5 mesylate
0 ImagesSynonyms: DX8951f-d5; Deuterated labeled Exatecan mesylateExatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
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Daunorubicin hydrochloride
0 ImagesSynonyms: Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochlorideDaunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
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Ciprofloxacin
0 ImagesSynonyms: Bay-09867Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
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Suramin sodium salt
0 ImagesSuramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
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Irinotecan hydrochloride
0 ImagesSynonyms: (+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.
