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TOP

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92

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16

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    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 .
    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 .
    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 .
    Tilatamig samrotecan
  • HY-174374

    Topoisomerase Cardiovascular Disease
    Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
    Topobexin
  • 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 .
    Puxitatug samrotecan
  • 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 .
    LMP744 hydrochloride
  • 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 .
    Topi MF-6
  • 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 .
    NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT hydrochloride
  • 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 .
    P5(PEG24)-VC-PAB-Exatecan
  • HY-122594

    Topoisomerase Cancer
    BNS-22 is a DNA topoisomerase II (TOP2) catalytic inhibitor with the IC50 values of 2.8 μM and 0.42 μM for human TOP2α and TOP2β, respectively. BNS-22 induces abnormal division and has anti-proliferative activity .
    BNS-22
  • HY-U00248

    MJ-III65; NSC706744

    Topoisomerase Cancer
    LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
    LMP744
  • HY-111630
    PluriSIn #2
    3 Publications Verification

    Topoisomerase Cancer
    PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs) .
    PluriSIn #2
  • 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 .
    (±)-Evodiamine
  • HY-168489

    Drug-Linker Conjugates for ADC Cancer
    OBI-992 drug-linker is a drug-linker conjugate composed of a TOP I inhibitor Exatecan (HY-13631) and a linker. OBI-992 drug-linker exhibits antitumor property in mouse models and can be used for synthesis of ADC OBI-992 .
    OBI-992 drug-linker
  • HY-116785

    DNA/RNA Synthesis Cancer
    BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
    BRD32048
  • HY-160857

    Estrogen Receptor/ERR Endocrinology
    TOP5668 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5668 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
    TOP5668
  • 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 .
    LMP517
  • HY-18350

    LMP776

    Topoisomerase Cancer
    Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities .
    Indimitecan
  • HY-118581
    Coralyne chloride
    1 Publications Verification

    Topoisomerase Cancer
    Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage . Coralyne chloride can be used for preparing?coralyne derivatives?as DNA binding fluorescent probes .
    Coralyne chloride
  • HY-13550

    NSC 196473; NSC 290813

    DNA/RNA Synthesis Cancer
    Ametantrone (NSC 196473) is an antitumor agent that intercalates into DNA and induces topoisomerase II (TOP2)-mediated DNA break .
    Ametantrone
  • HY-164143

    Topoisomerase Cancer
    T638 is a topoisomerase II (TOP2) inhibitor. T638 inhibits TOP2A activity with a IC50 of 0.7 uM. T638 strongly inhibits cancer cell growth .
    T638
  • HY-118911

    ATM/ATR Cancer
    ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
    ATM Inhibitor-10
  • 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) .
    Tilatamig
  • 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 .
    Top1 inhibitor 1
  • HY-RS14897

    Small Interfering RNA (siRNA) Others

    TOP2B Human Pre-designed siRNA Set A contains three designed siRNAs for TOP2B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TOP2B Human Pre-designed siRNA Set A
    TOP2B Human Pre-designed siRNA Set A
  • 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-RS14899

    Small Interfering RNA (siRNA) Others

    TOP3B Human Pre-designed siRNA Set A contains three designed siRNAs for TOP3B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    TOP3B Human Pre-designed siRNA Set A
    TOP3B Human Pre-designed siRNA Set A
  • HY-175700

    Topoisomerase Apoptosis Cancer
    YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .
    YCJ-02
  • HY-RS14902

    Small Interfering RNA (siRNA) Others

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

    TOPORS Human Pre-designed siRNA Set A
    TOPORS Human Pre-designed siRNA Set A
  • 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 .
    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 .
    DiPT-4
  • HY-123393

    Topoisomerase Others
    PNU-142586 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 .
    PNU-142586
  • 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 .
    Topovale
  • 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 .
    meso-Tetra(4-pyridyl)porphine
  • HY-160856

    TOP05300

    Estrogen Receptor/ERR Endocrinology
    TOP5300 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5300 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
    TOP5300
  • HY-175834

    Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin Cancer
    DNA/TOP2A-IN-1 is an inhibitor of DNA and TOP2A. DNA/TOP2A-IN-1 selectively binds to TOP2A, not TOP2B, and interacts with DNA and TOP2A to form a stable DM1-TOP2A-DNA ternary complex. DNA/TOP2A-IN-1 induces DNA damage, increases reactive oxygen species (ROS) and triggers apoptosis in triple-negative breast cancer (TNBC) cells. DNA/TOP2A-IN-1 disrupts microtubule distribution and induces cell cycle arrest. DNA/TOP2A-IN-1 shows strong antiproliferative activity and inhibits cell migration. DNA/TOP2A-IN-1 inhibits tumor growth and can be used for TNBC research .
    DNA/TOP2A-IN-1
  • HY-145852

    HDAC Topoisomerase Apoptosis Cancer
    Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis .
    Top/HDAC-IN-2
  • HY-160930

    p38 MAPK Src Syk Inflammation/Immunology
    TOP1288 is a narrow spectrum kinase inhibitor for P38α, Src and Syk kinase, with IC50 of 116nM, 24nM and 659nM, respectively. TOP1288 inhibits inflammatory cytokine release from inflamed biopsies and myofibroblasts .
    TOP1288
  • 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 .
    Topoisomerase I inhibitor 2
  • 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 .
    ZM484
  • HY-P4926

    Amyloid-β Neurological Disease
    Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
    Mca-SEVKMDAEFRK(Dnp)RR-NH2
  • HY-B2143

    Environmental Pollutants Biochemical Assay Reagents Bacterial Infection
    Montmorillonite is composed of two layers of co-top connected silicon oxygen tetrahedral sheet and one layer of co-edge connected aluminum (magnesium) oxygen (hydroxide) octahedral sheet, which consists of a 2:1 structure containing water of crystal. Montmorillonite can be used for large-scale industrial decontamination and can effectively remove harmful ions in sewage. Montmorillonite can also be used as a carrier of ionic antibacterial agents because of its exchangeable hydrated cations, which can adsorb bacteria .
    Montmorillonite
  • HY-176762

    Topoisomerase Infection Cancer
    TOP3B-IN-1 (NSC-260610) is a Topoisomerase IIIβ (TOP3B) inhibitor. TOP3B-IN-1 fails to induce the formation of TOP3B cleavage complexes (TOP3Bccs) with both DNA and RNA, and destabilizes TOP3Bccs. TOP3B-IN-1 can be used as a control compound for the development of inhibitors targeting TOP3B .
    TOP3B-IN-1
  • 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 .
    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 .
    Top1/2-IN-1
  • HY-178029

    Ribosomal S6 Kinase (RSK) Topoisomerase Apoptosis Autophagy Reactive Oxygen Species (ROS) Cancer
    RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma .
    RSK2/TOP2-IN-1
  • HY-125387

    Src Inflammation/Immunology
    TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
    TOP1210
  • HY-144654

    HDAC Topoisomerase Cancer
    HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy .
    HDAC/Top-IN-1
  • HY-145851

    HDAC Topoisomerase Apoptosis Cancer
    Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells .
    Top/HDAC-IN-1

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