2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Topoisomerase

Topoisomerase

Topoisomerase

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Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.

Topoisomerase Isoform Specific Products:

Topoisomerase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156849
    Exatecan-methylacetamide-OH
    		Inhibitor
    Exatecan-methylacetamide-OH (compound 6) is a Exatecan derivative with anticancer effects. Exatecan-methylacetamide-OH is an ADC cytotoxin that can be used to synthesize Antibody-Drug Conjugates (ADCs) (CN112125915A; compound 6).
    Exatecan-methylacetamide-OH
  • HY-160807
    DBM-GGFG-NH-O-CO-Exatecan
    		Inhibitor
    DBM-GGFG-NH-O-CO-Exatecan is an inhibitor for topoisomerase I. DBM-GGFG-NH-O-CO-Exatecan can be used as a drug-linker conjugate for synthesis of ADC molecule.
    DBM-GGFG-NH-O-CO-Exatecan
  • HY-150401
    Exatecan-amide-cyclopropanol
    		Inhibitor 98.57%
    Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively.
    Exatecan-amide-cyclopropanol
  • HY-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
    		Inhibitor 99.72%
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo.
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-13622
    Elomotecan hydrochloride
    		Inhibitor
    Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
    Elomotecan hydrochloride
  • HY-108969
    Pyrazoloacridine
    		Inhibitor 98.05%
    Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
    Pyrazoloacridine
  • HY-120574
    TH1338
    		Inhibitor 98.77%
    TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
    TH1338
  • HY-114668
    Camptothecin-20(S)-O-propionate
    		Inhibitor 99.55%
    Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor.
    Camptothecin-20(S)-O-propionate
  • HY-13704R
    SN-38 (Standard)
    		Inhibitor
    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).
    SN-38 (Standard)
  • HY-153031A
    Val-Cit-PAB-Exatecan TFA
    		Inhibitor 99.73%
    Val-Cit-PAB-Exatecan (Val-Cit-PAB-DX8951) TFA is a agent-linker conjugate for ADC. Val-Cit-PAB-Exatecan TFA is composed of a DNA topoisomerase I DX-8951 (HY-13631) and a cathepsin cleavable ADC linker.
    Val-Cit-PAB-Exatecan TFA
  • HY-B0356AS1
    Ciprofloxacin-13C3,15N monohydrochloride
    		Inhibitor 99.9%
    Ciprofloxacin-13C3,15N (Bay-09867-13C3,15N) monohydrochloride is 13C- and 15N-labeled Ciprofloxacin (monohydrochloride) (HY-B0356A).
    Ciprofloxacin-<sup>13</sup>C<sub>3</sub>,<sup>15</sup>N monohydrochloride
  • HY-13768
    Topotecan
    		Inhibitor
    Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
    Topotecan
  • HY-B0879
    Suramin
    		Inhibitor
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
    Suramin
  • HY-135867A
    NHC-triphosphate tetrasodium
    		Inhibitor
    NHC-triphosphate tetrasodium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form. NHC-triphosphate tetrasodium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-triphosphate tetrasodium
  • HY-147095A
    Val-Ala-PABC-Exatecan trifluoroacetate
    		Inhibitor 98.39%
    Val-Ala-PABC-Exatecan trifluoroacetate is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor, HY-13631). Val-Ala-PABC-Exatecan trifluoroacetate can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan.
    Val-Ala-PABC-Exatecan trifluoroacetate
  • HY-135867F
    NHC-diphosphate triammonium
    		Inhibitor 98.80%
    NHC-diphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form. NHC-diphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.
    NHC-diphosphate triammonium
  • HY-145397S
    (4-NH2)-Exatecan-d5
    		Inhibitor 98.62%
    (4-NH2)-Exatecan-d5 is a deuterated labeled (4-NH2)-Exatecan. (4-NH2)-Exatecan (compound A), a topoisomerase inhibitor, is a derivative of Exatecan. (4-NH2)-Exatecan can be used in the synthesis of antibody-drug conjugates (ADCs).
    (4-NH2)-Exatecan-d5
  • HY-164835
    VcMMAE-Deruxtecan
    		Inhibitor 98.10%
    VcMMAE-Deruxtecan is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule MMAE (HY-15162) (Microtubule inhibitor) and Exatecan (HY-13631) (DNA topoisomerase I inhibitor). VcMMAE-Deruxtecan can be used for ADC synthesis.
    VcMMAE-Deruxtecan
  • HY-157407
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
    		Inhibitor
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan is a drug-linker conjugate for ADC (ADC Cytotoxin: Exatecan).
    Cyclooctyne-O-amido-PEG4-VC-PAB-Gly-Gly-NH-O-CO-Exatecan
  • HY-164143
    T638
    		Inhibitor 98.61%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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