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. | Product Name | CAS No. | Information |
---|---|---|---|
H9038 |
(S)-Erypoegin K |
2055053-90-0 | (S)-Erypoegin K is an isoflavone isolated from Erythrina poeppigiana, is a novel inhibitor of topoisomerase IIα: Induction of G2 phase arrest in human gastric cancer cells.The IC50 of (S)-Erypoegin K for apoptotic cell death of HL-60 cells was 90 nM, which was much lower than many other antitumor drugs. |
H8615 |
Pyrazoloacridine |
99009-20-8 | Pyrazoloacridine (NSC 366140) is 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. |
H8381 |
Merbarone |
97534-21-9 | Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage. Merbarone is an anticancer agent. |
H2298 |
XR-5000 |
89459-25-6 | XR-5000 (Acridine Carboxamide) is an inhibitor of topoisomerase I and II for treatment of various types of cancers. |
H2297 |
Voreloxin |
175414-77-4 | A first-in-class anticancer quinolone derivative that intercalates DNA and inhibits Topoisomerase II; exhibits proliferation inhibition of AML cell lines MV4-11 and HL-60 with IC50 of 95 nM and 884 nM, respectively. |
H2296 |
SW-044248 |
522650-83-5 | SW-044248 is a novel selective inhibitor of Topoisomerase I; inhibits Top I differently from camptothecin; selectively toxic for some NSCLC cell lines. |
H2295 |
Indotecan |
915303-09-2 | Indotecan (LMP400) is an anticancer DNA Topoisomerase I (Top1) inhibitor. |
H2294 |
Indimitecan |
915360-05-3 | Indimitecan (LMP776, NSC 725776) is an anticancer DNA Topoisomerase I (Top1) inhibitor. |
H2292 |
Idarubicin hydrochloride |
57852-57-0 | An anthracycline antileukemic that inserts into DNA and prevents DNA unwinding by interfering with the enzyme Topoisomerase II in cancer cells; inhibits the proliferation of MCF-7 cells with IC50 of 0.1 uM; also induces histone eviction from chromatin. |
H2291 |
Idarubicin |
58957-92-9 | Idarubicin (4-Demethoxydaunorubicin;IMI-30;NSC 256439) is an anthracycline antileukemic that inserts into DNA and prevents DNA unwinding by interfering with the enzyme Topoisomerase II in cancer cells; inhibits the proliferation of MCF-7 cells with IC50 of 0.1 uM; also induces histone eviction from chromatin. |
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