Search Result
Results for "
DNA topoisomerase I inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
11
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N3488
-
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Topoisomerase
Bacterial
Fungal
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Infection
Cancer
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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 .
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- HY-16562
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(+)-Irinotecan; CPT-11; VAL-413(free base)
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Topoisomerase
Autophagy
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Cancer
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Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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-
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- HY-159783
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- HY-16562S1
-
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Isotope-Labeled Compounds
Topoisomerase
Autophagy
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Cancer
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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 .
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-
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- HY-16562S
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(+)-Irinotecan-d10; CPT-11-d10; VAL-413-d10
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Topoisomerase
Autophagy
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Cancer
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Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-162587
-
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Topoisomerase
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Cancer
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Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors .
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- HY-156723
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Topoisomerase
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Cancer
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9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research .
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- HY-143265
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Topoisomerase
Apoptosis
Caspase
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Cancer
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Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect .
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- HY-143266
-
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
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- HY-144774
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Topoisomerase
DNA/RNA Synthesis
Apoptosis
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Cancer
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Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
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- HY-146437
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases .
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- HY-N15319
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Canangine
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Topoisomerase
Fungal
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Infection
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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 .
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- HY-125930A
-
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Topoisomerase
DNA/RNA Synthesis
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Cancer
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T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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- HY-125930
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Topoisomerase
DNA/RNA Synthesis
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Cancer
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T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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- HY-16562R
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(+)-Irinotecan (Standard); CPT-11 (Standard); VAL-413(free base) (Standard)
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Reference Standards
Topoisomerase
Autophagy
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Cancer
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Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-119892
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NSC 320846; BAY-H 2049
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Topoisomerase
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Cancer
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Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
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- HY-161385
-
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Topoisomerase
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Cancer
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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 .
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- HY-N10115
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- HY-19825
-
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Topoisomerase
ADC Payload
Antibiotic
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Cancer
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Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
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- HY-N4329
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Topoisomerase
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Others
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Nidulalin A is a DNA topoisomerase II inhibitor with an IC50 of 2.2 μM. Nidulalin A has an IC50 of 172 μM for DNA topoisomerase I. Nidulalin A has certain cytotoxicity .
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- HY-143402
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Topoisomerase
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Cancer
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Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
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- HY-100777
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Topoisomerase
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Cancer
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DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
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- HY-120185
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UCT-1003
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Topoisomerase
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Infection
Cancer
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Saintopin is an antitumor antibiotic. Saintopin is also an inhibitor of DNA topoisomerases I and II. Saintopin induces DNA cleavage .
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- HY-13758
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BMS-247615
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Topoisomerase
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Cancer
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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- HY-13758A
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BMS-247615 dihydrochloride
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Topoisomerase
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Cancer
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TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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- HY-168739
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Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
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Cancer
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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 .
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- HY-13618
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J 107088; PF 804950
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Topoisomerase
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Cancer
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Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
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- HY-13565
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NSC 655649; BMS 181176; BMY 27557
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Topoisomerase
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Cancer
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Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
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- HY-100777R
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Topoisomerase
Reference Standards
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Cancer
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DACA (Standard) is the analytical standard of DACA. This product is intended for research and analytical applications. DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
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- HY-U00248
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MJ-III65; NSC706744
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Topoisomerase
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Cancer
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LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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- HY-U00248A
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MJ-III65 hydrochloride; NSC706744 hydrochloride
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Topoisomerase
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Cancer
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LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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- HY-N2063
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Topoisomerase
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Others
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12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM .
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- HY-N10367
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Topoisomerase
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Cancer
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Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity .
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- HY-13631
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DX-8951
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ADC Payload
Topoisomerase
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Cancer
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Exatecan (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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- HY-169509
-
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PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
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Cancer
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Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
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- HY-13631A
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DX8951f
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ADC Payload
Topoisomerase
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Cancer
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Exatecan 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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- HY-42487
-
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ADC Payload
Topoisomerase
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Cancer
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Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects .
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- HY-121309
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Adriamycin aglycone; Adriamycinone
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Endogenous Metabolite
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Cancer
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Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-N2198
-
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Topoisomerase
Apoptosis
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Cancer
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Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
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- HY-13631P
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DX-8951 mesylate dihydrate
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ADC Payload
Topoisomerase
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Cancer
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Exatecan (DX-8951) mesylate dihydrate 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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- HY-13744
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RFS 2000; 9-Nitrocamptothecin
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Topoisomerase
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Cancer
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Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells .
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- HY-160774
-
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
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Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC .
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- HY-158230
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Topoisomerase
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Cancer
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SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells .
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- HY-16055
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AR-67; DB 67
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Topoisomerase
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Cancer
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Silatecan (AR-67; DB 67) is a Camptothecin (HY-16560) analogue with improved stability and lipophilicity. Silatecan is an inhibitor for topoisomerase I, that inhibits the DNA replication and transcription, and exhibits antitumor and radiosensitizing activities
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- HY-145078
-
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Drug-Linker Conjugates for ADC
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Cancer
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PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5 .
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- HY-121309S
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Adriamycin aglycone-d3; Adriamycinone-d3
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Endogenous Metabolite
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Cancer
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Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human?DNA topoisomerase I?and?topoisomerase II?inhibitor with?IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-161970
-
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Topoisomerase
Apoptosis
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Cancer
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XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
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- HY-13631D
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Exatecan derivative for ADC
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Topoisomerase
ADC Payload
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Cancer
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Dxd (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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-
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- HY-156848
-
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Drug-Linker Conjugates for ADC
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Cancer
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Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
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- HY-153013
-
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Drug-Linker Conjugates for ADC
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Cancer
|
SN38-COOH is used for the synthesis of antibody-drug conjugates (ADCs). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis .
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- HY-101647
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RP 60475
|
Topoisomerase
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Cancer
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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 10 5 /M) and thereby increases the length of linear DNA .
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- HY-121309R
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Adriamycin aglycone (Standard); Adriamycinone (Standard)
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Reference Standards
Endogenous Metabolite
|
Cancer
|
Doxorubicinone (Standard) is the analytical standard of Doxorubicinone. This product is intended for research and analytical applications. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-B1099
-
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
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- HY-13566
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CKD-602 free base
|
Topoisomerase
Apoptosis
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Cancer
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Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
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- HY-13631AS1
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-
- HY-49556
-
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Topoisomerase
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Cancer
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(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate reactant in the synthesis of Camptothecin (HY-16560). Camptothecin is an inhibitor of the DNA topoisomerase Topo I, withIC50=679 nM .
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- HY-15142A
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Hydroxydaunorubicin
|
ADC Payload
Antibiotic
Bacterial
Topoisomerase
AMPK
HIV
Autophagy
Mitophagy
Apoptosis
HBV
|
Infection
Cancer
|
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC50 of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy . Doxorubicin inhibits human DNA topoisomerase I with an IC50 of 0.8 μM .
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- HY-164835
-
-
- HY-164836
-
-
- HY-148668A
-
-
- HY-13631R
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DX-8951 (Standard)
|
ADC Payload
Reference Standards
Topoisomerase
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Cancer
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Exatecan (Standard) is the analytical standard of Exatecan. This product is intended for research and analytical applications. Exatecan (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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- HY-148668
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SHR-A1811 Drug-linker
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
|
MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM) .
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-
- HY-101647A
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RP 60475 dimesylate
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Topoisomerase
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Cancer
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Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
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-
- HY-174151
-
|
Topoisomerase
Apoptosis
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Cancer
|
XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
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-
- HY-175203
-
|
Topoisomerase
ADC Payload
|
Cancer
|
Topi MF-6 is a DNA topoisomerase I (Top1) inhibitor. Topi MF-6 has superior cytotoxicity against gastrointestinal cancer cells. Topi MF-6 can be used as an ADC payload .
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-
- HY-48878
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan analog 36 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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-
- HY-13631AG
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DX8951f
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan 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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- HY-164647
-
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Drug-Linker Conjugates for ADC
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Cancer
|
Val-Ala-PABC-N(Mesylpropane)-Exatecan is an agent-linker conjugate for ADC. Val-Ala-PABC-N(Mesylpropane)-Exatecan is a Exatecan (a DNA topoisomerase I inhibitor) d with cleavable Val-Ala-PABC-N(Mesylpropane) linker .
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-
- HY-136170
-
MC-SN38
2 Publications Verification
|
Drug-Linker Conjugates for ADC
|
Cancer
|
MC-SN38 is a agent-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody agent conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks .
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-
- HY-43565
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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-
- HY-49861
-
|
ADC Payload
Topoisomerase
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Cancer
|
Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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-
- HY-43565B
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2 .2 μM (0 .975 μg/mL) for use in cancer research .
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-
- HY-400316
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan intermediate 8 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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-
- HY-158137
-
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Drug-Linker Conjugates for ADC
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Cancer
|
Val-Cit-PAB-DEA-Dxd (compound 81) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Dxd (DNA topoisomerase I inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis .
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- HY-13631DS
-
Exatecan-d5 derivative for ADC
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Topoisomerase
ADC Payload
|
Cancer
|
Dxd-d5 is a deuterium labeled Dxd. Dxd 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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-
- HY-156755
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for ADC. Propargyl-PEG4-GGFG-DXd contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
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-
- HY-121309S1
-
Adriamycin aglycone-13C,d3; Adriamycinone-13C,d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cancer
|
Doxorubicinone- 13C,d3 (Adriamycin aglycone- 13C,d3) is 13C labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
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-
- HY-15142
-
Hydroxydaunorubicin hydrochloride; ADR
|
Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
|
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 .
|
-
- HY-131057
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-N11536
-
|
Topoisomerase
Apoptosis
|
Cancer
|
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
|
-
- HY-13704
-
7-Ethyl-10-hydroxycamptothecin
|
Drug Metabolite
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
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) .
|
-
- HY-18351A
-
LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-B1099R
-
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
Hycanthone (Standard) is the analytical standard of Hycanthone. This product is intended for research and analytical applications. Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
|
-
- HY-125331
-
|
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 .
|
-
- HY-13631AS
-
DX8951f-d5; Deuterated labeled Exatecan mesylate
|
Isotope-Labeled Compounds
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan-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 .
|
-
- HY-43565C
-
|
Drug Intermediate
|
Cancer
|
(1S,9R)-Ac-Exatecan is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-156686
-
|
ADC Payload
Topoisomerase
|
Cancer
|
NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-16560
-
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 .
|
-
- HY-171124
-
AZD9592
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer .
|
-
- HY-18351
-
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-147270
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity .
|
-
- HY-44369
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan Intermediate 6 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 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-107096
-
TP3076
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-43564
-
|
ADC Payload
Topoisomerase
|
Cancer
|
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).
|
-
- HY-13631F
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNA topoisomerase I inhibitor that can be used in cancer research .
|
-
- HY-13566R
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Belotecan (Standard) is the analytical standard of Belotecan. This product is intended for research and analytical applications. Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
|
-
- HY-46081
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan Intermediate 3 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 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-164792
-
-
- HY-45157
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Exatecan Intermediate 7 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 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-15142R
-
Hydroxydaunorubicin hydrochloride (Standard); ADR (Standard)
|
Reference Standards
Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
|
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 .
|
-
- HY-168285
-
-
- HY-107096B
-
TP3076 TFA
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-13704S
-
NK012-d3
|
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
|
-
- HY-156376
-
|
Cuproptosis
Apoptosis
Topoisomerase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu 2+ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer .
|
-
- HY-171580
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
|
-
- HY-147307
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer .
|
-
- HY-114233
-
MC-GGFG-DX8951
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC) .
|
-
- HY-122532
-
|
Histone Methyltransferase
|
Cancer
|
Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection .
|
-
- HY-16560S
-
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 .
|
-
- HY-13631I
-
(1S,9R)-DX8951f
|
ADC Payload
Topoisomerase
|
Cancer
|
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
|
-
- HY-79490
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells .
|
-
- HY-W046353
-
o-Methoxycinnamaldehyde
|
Apoptosis
NF-κB
Topoisomerase
Mitochondrial Metabolism
Caspase
|
Cancer
|
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-116926
-
|
Antibiotic
Bacterial
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Infection
Cancer
|
Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1 .
|
-
- HY-B0147
-
Pefloxacinium
|
Antibiotic
Bacterial
Parasite
DNA/RNA Synthesis
Topoisomerase
|
Infection
Inflammation/Immunology
|
Pefloxacin is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-148696A
-
|
ADC Payload
Topoisomerase
|
Cancer
|
Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro .
|
-
- HY-P99843
-
|
TROP2
ADC Antibody
|
Cancer
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
- HY-13631J
-
(1R,9R)-DX8951f
|
ADC Payload
Topoisomerase
|
Cancer
|
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research .
|
-
- HY-13704R
-
7-Ethyl-10-hydroxycamptothecin (Standard)
|
Drug Metabolite
Reference Standards
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
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) .
|
-
- HY-16560R
-
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.
|
-
- HY-B0147S
-
Pefloxacinium-d5
|
Antibiotic
Bacterial
Isotope-Labeled Compounds
|
Others
|
Pefloxacin-d5 is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-N0095
-
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
|
-
- HY-164152
-
|
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) .
|
-
- HY-164152A
-
|
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) .
|
-
- HY-162472
-
|
ATM/ATR
DNA-PK
|
Cancer
|
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-134723
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
|
-
- HY-128943
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
|
-
- HY-W046353R
-
o-Methoxycinnamaldehyde (Standard)
|
Reference Standards
Apoptosis
NF-κB
Mitochondrial Metabolism
Caspase
Topoisomerase
|
Cancer
|
2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-163099
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
P5(PEG24)-VC-PAB-Exatecan (LP5) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG24)-VC-PAB-Exatecan can be used for the research of tumor .
|
-
- HY-173625
-
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
|
-
- HY-156513
-
7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)
|
ADC Payload
|
Cancer
|
ZD06519 (7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)) is a camptothecin (HY-16560) analogue and a topoisomerase I inhibitor. ZD06519 is an ADC cytotoxin with a strong bystander effect, inhibiting a variety of malignancies such as HER2-positive and FRα-overexpressing tumors. ZD06519 inhibits DNA cleavage, relaxation, and reconnection processes, inducing tumor cell death. ZD06519 can be used for ADC synthesis and cancer research .
|
-
- HY-173703
-
|
Topoisomerase
Drug Intermediate
|
Cancer
|
β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers .
|
-
- HY-N0095S
-
10-HCPT-d5; 10-Hydroxycamptothecin-d5
|
Isotope-Labeled Compounds
Apoptosis
Topoisomerase
|
Cancer
|
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
|
-
- HY-128946
-
|
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 .
|
-
- HY-162805
-
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
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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) .
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- HY-N0095R
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10-HCPT (Standard); 10-Hydroxycamptothecin (Standard)
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Reference Standards
Topoisomerase
Apoptosis
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Cancer
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(S)-10-Hydroxycamptothecin (Standard) is the analytical standard of (S)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
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- HY-118899
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Endogenous Metabolite
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Cancer
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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 .
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- HY-173634
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
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Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639) .
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Cat. No. |
Product Name |
Type |
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- HY-13631AG
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DX8951f (GMP)
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Fluorescent Dye
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan 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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Cat. No. |
Product Name |
Type |
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- HY-13631AG
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DX8951f (GMP)
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Biochemical Assay Reagents
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan 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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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99843
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TROP2
ADC Antibody
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Cancer
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Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
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- HY-164152
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Antibody-Drug Conjugates (ADCs)
Topoisomerase
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Cancer
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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) .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-16562S1
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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 .
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- HY-16562S
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Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-13631DS
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Dxd-d5 is a deuterium labeled Dxd. Dxd 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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- HY-13631AS
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Exatecan-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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- HY-13704S
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SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
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- HY-16560S
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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 .
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- HY-B0147S
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Pefloxacin-d5 is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
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- HY-121309S
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Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human?DNA topoisomerase I?and?topoisomerase II?inhibitor with?IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-13631AS1
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Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
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- HY-121309S1
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Doxorubicinone- 13C,d3 (Adriamycin aglycone- 13C,d3) is 13C labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
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- HY-N0095S
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(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
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Cat. No. |
Product Name |
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Classification |
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- HY-164792
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DBCO
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DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
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- HY-134723
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ADC Synthesis
DBCO
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DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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- HY-163099
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Alkynes
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P5(PEG24)-VC-PAB-Exatecan (LP5) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG24)-VC-PAB-Exatecan can be used for the research of tumor .
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- HY-173625
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Alkynes
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P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
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