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Isoforms Recommended: Topo I
Results for "

TOP1

" in MedChemExpress (MCE) Product Catalog:

39

Inhibitors & Agonists

1

Inhibitory Antibodies

5

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2

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4

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 [1]. 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-148819

    ADC Payload Topoisomerase Cancer
    NH2-bicyclopentane-7-MAD-MDCPT (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT is used in research on lung adenocarcinoma and melanoma [1].
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
  • HY-153278

    CDK7-IN-21

    CDK DNA/RNA Synthesis c-Myc Early 2 Factor (E2F) Topoisomerase Cancer
    Q901 (CDK7-IN-21) is a selective and potent CDK7 inhibitor with an IC50 of 10 nM. Q901 disrupts MYC and E2FTOP1-DPCs and sensitizes tumor to TOP1 inhibitors by suppressing RNAPII transition from initiation to elongation. Q901 can inhibit tumor growth and significantly enhances tumor growth inhibition combined with TOP1 inhibitors. Q901 can be used for the research of cancer, such as colon cancer and lung cancer [1].
    Q901
  • HY-164734

    R-DXd; DS-6000

    Antibody-Drug Conjugates (ADCs) Cancer
    Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC50 of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, Chk1 phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma [1].
    Raludotatug Deruxtecan
  • HY-171124

    AZD9592

    Antibody-Drug Conjugates (ADCs) EGFR c-Met/HGFR Topoisomerase DNA/RNA Synthesis Cancer
    Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research [1] .
    Tilatamig samrotecan
  • HY-175203

    Topoisomerase ADC Payload Cancer
    Topi MF-6 is a DNA topoisomerase I (Top1) inhibitor. Topi MF-6 can be used as an ADC payload [1].
    Topi MF-6
  • HY-U00248A

    MJ-III65 hydrochloride; NSC706744 hydrochloride

    Topoisomerase Cancer
    LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity [1].
    LMP744 hydrochloride
  • HY-148819A

    ADC Payload Topoisomerase Cancer
    NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma [1].
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
  • HY-171689

    AZD 8205; P-Sam

    Antibody-Drug Conjugates (ADCs) Topoisomerase Cancer
    Puxitatug samrotecan (AZD 8205) is a B7-H4-directed antibody-drug conjugate (ADC) bearing a Topoisomerase I inhibitor (TOP1i) payload. Puxitatug samrotecan improves HR +/HER2 - breast cancer [1] .
    Puxitatug samrotecan
  • HY-163099

    Drug-Linker Conjugates for ADC Topoisomerase Apoptosis Cancer
    P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers [1].
    P5(PEG24)-VC-PAB-Exatecan
  • HY-N0114A
    (±)-Evodiamine
    1 Publications Verification

    Topoisomerase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis [1].
    (±)-Evodiamine
  • HY-U00248

    MJ-III65; NSC706744

    Topoisomerase Cancer
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity [1].
    LMP744
  • HY-126142

    Topoisomerase ADC Payload Cancer
    Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM [1].
    Top1 inhibitor 1
  • HY-160005

    NSC 781517

    Topoisomerase DNA/RNA Synthesis Cancer
    LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer [1] .
    LMP517
  • HY-18350

    LMP776

    Topoisomerase Cancer
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities [1].
    Indimitecan
  • HY-P990947

    AZD9592 Antibody

    ADC Antibody EGFR Cancer
    Tilatamig (AZD9592 Antibody) is a human antibody of the Ig (G1-κ_G1-λ2) subtype that targets EGFR/MET. Tilatamig conjugates with the Top1 inhibitor AZ14170133 (HY-145399) to form the antibody-drug conjugate (ADC) Tilatamig samrotecan (HY-171124) (AZD9592). Tilatamig accurately targets NSCLC models including EGFR-mutant, EGFR-wildtype, and EGFR tyrosine kinase inhibitor-treated ones, and its activity correlates with high expression of EGFR, c-MET and SLFN11. Tilatamig is available for in vivo anti-tumor studies in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) [1].
    Tilatamig
  • HY-RS14891

    Small Interfering RNA (siRNA) Topoisomerase Others

    Top1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Top1 Mouse Pre-designed siRNA Set A
    Top1 Mouse Pre-designed siRNA Set A
  • HY-RS14890

    Small Interfering RNA (siRNA) Topoisomerase Others

    TOP1 Human Pre-designed siRNA Set A contains three designed siRNAs for TOP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TOP1 Human Pre-designed siRNA Set A
    TOP1 Human Pre-designed siRNA Set A
  • HY-RS14892

    Small Interfering RNA (siRNA) Topoisomerase Others

    Top1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Top1 Rat Pre-designed siRNA Set A
    Top1 Rat Pre-designed siRNA Set A
  • HY-W008874

    Topoisomerase Cancer
    meso-Tetra(4-pyridyl)porphine (Compound 10) is a porphyrin derivative. meso-Tetra(4-pyridyl)porphine is a weak inhibitor of human topoisomerase I (Top1) with an EC50 value greater than 50 µM. meso-Tetra(4-pyridyl)porphine can be used in tumor research [1].
    meso-Tetra(4-pyridyl)porphine
  • HY-153278A

    CDK7-IN-21 TFA

    CDK DNA/RNA Synthesis c-Myc Early 2 Factor (E2F) Topoisomerase Cancer
    Q901 (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 [1].
    Q901 TFA
  • HY-149348

    Topoisomerase PARP Apoptosis Cancer
    DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance [1].
    DiPT-4
  • HY-118942

    ARC 111

    Topoisomerase Cancer
    Topovale (ARC 111) is a topoisomerase I inhbitor. Topovale is an antitumor agent, and shows low nM cytotoxicity against a panel of cancer cells. Topovale induces reversible topoisomerase I (TOP1) cleavage complexes in tumor cells [1].
    Topovale
  • HY-143265

    Topoisomerase Apoptosis Caspase Cancer
    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 [1].
    Topoisomerase I inhibitor 2
  • HY-RS14893

    Small Interfering RNA (siRNA) Others

    TOP1MT Human Pre-designed siRNA Set A contains three designed siRNAs for TOP1MT gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TOP1MT Human Pre-designed siRNA Set A
    TOP1MT Human Pre-designed siRNA Set A
  • HY-178036

    MDM-2/p53 Topoisomerase Bcl-2 Family Caspase Cyclin G-associated Kinase (GAK) Cancer
    ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research [1].
    ZM484
  • HY-159935

    Topoisomerase Apoptosis Cancer
    Top1-IN-2 (Compound 1a) is a topoisomerase 1 (Top1) inhibitor. Top1-IN-2 inhibits P-gp resistant tumor cells growth and induces cell apoptosis [1].
    Top1-IN-2
  • HY-161957

    Topoisomerase Cancer
    Top1/2-IN-1 (compound 23) is an orally available dual inhibitor of Top1/2 with antiproliferative activity. Top1/2-IN-1 damages DNA with increased levels of reactive oxygen species, inducing apoptosis and cell cycle arrest in cancer cells. Top1/2-IN-1 exhibits in vivo antitumor activity in xenograft models [1].
    Top1/2-IN-1
  • HY-133219

    Topoisomerase Cancer
    Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells [1].
    Guajadial C
  • HY-N0114AR

    Topoisomerase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    (±)-Evodiamine (Standard) is the analytical standard of (±)-Evodiamine. This product is intended for research and analytical applications. (±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis [1].
    (±)-Evodiamine (Standard)
  • HY-181080

    Topoisomerase DNA/RNA Synthesis Apoptosis Cancer
    TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer [1].
    TOP1/TDP1-IN-1
  • HY-18350A

    LMP776 hydrochloride

    Topoisomerase Cancer
    Indimitecan hydrochloride is a topoisomerase I (Top1) inhibitor with anticancer activities [1].
    Indimitecan hydrochloride
  • HY-16560B

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

    Topoisomerase Drug Isomer Others
    (R)-Camptothecin is an enantiomer of Camptothecin (CPT), is inactive as an inhibitor of the DNA religation reaction and consequently do not poison Top1 [1].
    (R)-Camptothecin
  • HY-168739

    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 [1].
    Topoisomerase I inhibitor 17
  • HY-146437

    Topoisomerase Cancer
    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 [1].
    Topoisomerase I inhibitor 6
  • HY-N15249

    Isovalerylspiramycin I; Shengjimycin E

    Topoisomerase DNA/RNA Synthesis Checkpoint Kinase (Chk) Apoptosis Bacterial Infection Cancer
    4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection [1] .
    4
  • HY-144794

    Apoptosis EGFR FAK Cancer
    EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis [1].
    EGFR-IN-46
  • HY-180555

    PROTACs STING Inflammation/Immunology Cancer
    SN38-(PEG)2-Pom-α is a selective PROTAC RPL15 degrader. SN38-(PEG)2-Pom-α induces ubiquitin-mediated degradation of RPL15 without affecting TOP1. SN38-(PEG)2-Pom-α induces damage-associated molecular pattern (DAMP) secretion from cancer cells, which activated cGAS-STING signaling in dendritic cells. SN38-(PEG)2-Pom-α enhances anti-PD-1 immunotherapy in a murine melanoma tumor model expressing human CRBN. SN38-(PEG)2-Pom-α can be used for melanoma research [1].
    SN38-(PEG)2-Pom-α
  • HY-W654323

    Topoisomerase Drug Metabolite Others
    PNU-142586 sodiu) is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism [1].
    PNU-142586 sodium

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