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-N0275R
    (±)-10-Hydroxycamptothecin (Standard)
    		Inhibitor
    (±)-10-Hydroxycamptothecin (Standard) is the analytical standard of (±)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.
    (±)-10-Hydroxycamptothecin (Standard)
  • HY-180767
    Azithromycin-amide-C3-amide-quinoxaline
    		Inhibitor
    Azithromycin-amide-C3-amide-quinoxaline (Compound 5f) is an Azithromycin (HY-17506) derivative and antibacterial agent. Azithromycin-amide-C3-amide-quinoxaline inhibits topoisoisomerase I with an IC50 of 120.7 μM. Azithromycin-amide-C3-amide-quinoxaline interacts with 70S E. coli ribosome with a Kd of 0.8 nM. Azithromycin-amide-C3-amide-quinoxaline inhibits bacterial translation with an IC50 of 0.7 μM. Azithromycin-amide-C3-amide-quinoxaline shows antibacterial potency against S. pneumonia ATCC 49619, S. aureus ATCC 29213, E. faecalis ATCC 29212 with MICs of 0.06 μg/mL, 2 μg/mL, 0.5 μg/mL, respectively. Azithromycin-amide-C3-amide-quinoxaline exhibits anticancer activity against prostate cancer, colon cancer.
    Azithromycin-amide-C3-amide-quinoxaline
  • HY-W700069
    Gatifloxacin-d4
    		Inhibitor
    Gatifloxacin-d4 (AM-1155-d4) is the deuterium labeled Gatifloxacin (HY-10581). Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50 = 13.8 μg/mL for S. aureus topoisomerase IV) and E.coli DNA gyrase (IC50 = 0.109 μg/mL). Gatifloxacin can be used for the study of bacterial conjunctivitis in vivo.
    Gatifloxacin-d<sub>4</sub>
  • HY-100620R
    RPR121056 (Standard)
    		Inhibitor
    RPR121056 (Standard) is the analytical standard of RPR121056. This product is intended for research and analytical applications. RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE[1].
    RPR121056 (Standard)
  • HY-42487S1
    Exatecan Intermediate 1-d2
    Exatecan Intermediate 1-d2 is the deuterium labeled Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
    Exatecan Intermediate 1-d<sub>2</sub>
  • HY-13725AR
    Pirarubicin Hydrochloride (Standard)
    		Inhibitor
    Pirarubicin (Hydrochloride) (Standard) is the analytical standard of Pirarubicin (Hydrochloride). This product is intended for research and analytical applications. Pirarubicin Hydrochloride is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.
    Pirarubicin Hydrochloride (Standard)
  • HY-13562S
    Banoxantrone-d12
    Banoxantrone-d12 is the deuterium labeled banoxantrone. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
    Banoxantrone-d<sub>12</sub>
  • HY-13562AS
    Banoxantrone-d12 dihydrochloride
    Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor.
    Banoxantrone-d<sub>12</sub> dihydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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