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  2. Cell Cycle/DNA Damage
  3. Topoisomerase

Topoisomerase

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.

Cat. No. Nombre del producto Efecto Pureza Chemical Structure
  • HY-13502R
    Mitoxantrone (Standard)
    Inhibitor
    Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone (Standard)
  • HY-133219
    Guajadial C
    Inhibitor
    Guajadial C is a Top1 catalytic inhibitor that delays Top1 poison-mediated DNA damage. Guajadial C shows cytotoxicity against cancer cells.
    Guajadial C
  • HY-13622B
    Elomotecan TFA
    Inhibitor
    Elomotecan TFA is a potent inhibitor of topoisomerases I and II. Elomotecan TFA is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan TFA reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
    Elomotecan TFA
  • HY-13727AR
    Pixantrone (Standard)
    Inhibitor
    Pixantrone (Standard) is the analytical standard of Pixantrone. This product is intended for research and analytical applications. Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
    Pixantrone (Standard)
  • HY-101775
    9-Hydroxyellipticin
    Inhibitor
    9-hydroxyellipticine is an inhibitor of Topo II and RyR, exhibiting high affinity for DNA with a Pka value of 9.8 at pH 7.4. It has antitumor, antioxidant, and catecholamine-releasing activities, with IC50 values of 1.6 μM and 1.2 μM for Hela S-3 and 293T cells, respectively. It also demonstrates anticancer effects in L1210 leukemia mice.
    9-Hydroxyellipticin
  • HY-18626
    NK 314
    Inhibitor
    NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM.
    NK 314
  • HY-123363
    Tafluposide
    Inhibitor
    Tafluposide (F-11782) is a DNA topoisomerase inhibitor. Tafluposide has antitumor activity.
    Tafluposide
  • HY-B0356S2
    Ciprofloxacin-d4
    Inhibitor
    Ciprofloxacin-d4 (Bay-09867-d4) is deuterium labeled Ciprofloxacin. Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
    Ciprofloxacin-d<sub>4</sub>
  • HY-10581CR
    Gatifloxacin sesquihydrate (Standard)
    Inhibitor
    Gatifloxacin (sesquihydrate) (Standard) is the analytical standard of Gatifloxacin (sesquihydrate). This product is intended for research and analytical applications. Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate 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 sesquihydrate can be used to treat bacterial conjunctivitis?in vivo.
    Gatifloxacin sesquihydrate (Standard)
  • HY-134290
    8-Chloro-ATP
    Inhibitor
    8-Chloro-ATP, an ATP (HY-B2176) analog, is a topoisomerase II (Topo II) inhibitor. 8-Chloro-ATP inhibits DNA synthesis and induces DNA double-stranded breaks (DSBs). 8-Chloro-ATP inhibits Topo II-catalyzed ATP hydrolysis.
    8-Chloro-ATP
  • 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-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)
Cat. No. Nombre del producto / Synonyms Species Source
Cat. No. Nombre del producto / Synonyms Application Reactivity

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