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-10581R
    Gatifloxacin (Standard)
    		Inhibitor
    Gatifloxacin (Standard) is the analytical standard of Gatifloxacin. This product is intended for research and analytical applications. 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 to treat bacterial conjunctivitis in vivo.
    Gatifloxacin (Standard)
  • HY-A0170R
    Trovafloxacin (Standard)
    		Inhibitor
    Trovafloxacin (Standard) is the analytical standard of Trovafloxacin. This product is intended for research and analytical applications. Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
    Trovafloxacin (Standard)
  • HY-164271
    10-Boc-SN-38
    		Inhibitor
    10-Boc-SN-38 is a tert-butyloxycarbonyl (Boc)-protected form of SN-38 (HY-13704). SN-38 is the active metabolite of Irinotecan (HY-16562).
    10-Boc-SN-38
  • HY-132561S
    RPR121056-d3
    RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (HY-16562), 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.
    RPR121056-d3
  • HY-101775AR
    9-Hydroxyellipticine hydrochloride (Standard)
    		Inhibitor
    9-Hydroxyellipticine (hydrochloride) (Standard) is the analytical standard of 9-Hydroxyellipticine (hydrochloride). This product is intended for research and analytical applications. 9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC50 values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively.
    9-Hydroxyellipticine hydrochloride (Standard)
  • HY-15753AR
    Ellipticine hydrochloride (Standard)
    		Inhibitor
    Ellipticine (hydrochloride) (Standard) is the analytical standard of Ellipticine (hydrochloride). This product is intended for research and analytical applications. Ellipticine (NSC 71795) hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.
    Ellipticine hydrochloride (Standard)
  • HY-156462
    Topoisomerase I inhibitor 9
    		Inhibitor
    Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM.
    Topoisomerase I inhibitor 9
  • HY-W653896
    Alternariol-d2
    		Inhibitor
    Alternariol-d2 is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.
    Alternariol-d<sub>2</sub>
  • HY-N0716
    Berberine
    		Inhibitor
    Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.
    Berberine
  • HY-10982R
    Amonafide (Standard)
    		Inhibitor
    Amonafide (Standard) is the analytical standard of Amonafide. This product is intended for research and analytical applications. Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide (Standard)
  • HY-118726
    Luotonin F
    		Inhibitor
    Luotonin F is an alkaloid found in the aerial parts of the P. nigellastrum Bunge. Luotonin F shows cytotoxic activity against mouse leukemia P-388 cells by inhibiting human topoisomerase II.
    Luotonin F
  • HY-118379
    NU/ICRF 500
    		Inhibitor
    NU/ICRF 500 is a topo II catalytic inhibitor which increases CREST negative micronuclei in human lymphocytes.
    NU/ICRF 500
  • HY-16742B
    Gepotidacin mesylate hydrate
    		Inhibitor 99.62%
    Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial type II topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase.
    Gepotidacin mesylate hydrate
  • 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-118942
    Topovale
    		Inhibitor 99.94%
    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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Topoisomerase Isoform Comparison

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