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[1][2][3].
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK[1].
Flumequine-13C3 is the 13C3 labeled Flumequine. Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).
GGFG-amide-glycol-amide-Exatecan (Intermediate 2) is an Exatecan (HY-13631) derivative and can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
TP3011 is a potent topoisomerase-1 inhibitor and is the active metabolite converted from TP3076 by aldehyde oxidase 1 (AOX1)[1]. TP3011 has robust anti-tumor activities against cancer cell lines[2].
Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives.9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research[1].
Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research[1][2][3].
Br-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT (Formula V) is a drug-linker conjugate that composed of a potent topoisomerase I inhibitor and a linker to make antibody drug conjugate (ADC)[1].
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].
Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugstarget: DNA topoisomerase IIn vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest. PF (40 ug/mL, 24 hr) significantly induced about 10 folds of cell deaths and growth arrest in S-phase than the control group.
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity[1].
Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively[1].
Murrayanol is a natural carbazole alkaloid with a variety of biological activities. Murrayanol shows anti-inflammatory, topoisomerase I and topoisomerase II (Topoisomerase) inhibition activities. Murrayanol also as a mosquitocidal and antimicrobial[1].
Ac-Exatecan is acetylated Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM)[1].
RPR121056-d3 is the deuterium labeled RPR121056. RPR121056 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][2].
TP0480066 is a selective topoisomerase II inhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea[1][2].
Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer[1].
Epirubicin (hydrochloride) is a semisynthetic L-arabino derivative of doxorubicin, and an antineoplastic agent by inhibiting Topoisomerase.
HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1].
Levofloxacin ((-)-Ofloxacin) sodium is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin sodium inhibits the DNA gyrase and topoisomerase IV. Levofloxacin sodium can be used for chronic periodontitis, airway inflammation and BK Viremia research. Levofloxacin sodium shows anti-orthopoxvirus activity[1][2][3][4][5].
Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis[1].
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor[1][2].
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity[1][2].
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition[1].
Amsacrine is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
Levofloxacin ((-)-Ofloxacin) hydrochloride is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria. Levofloxacin hydrochloride inhibits the DNA gyrase and topoisomerase IV. Levofloxacin hydrochloride can be used for chronic periodontitis, airway inflammation and BK Viremia research[1][2][3][4].
Indotecan (LMP-400) is a potent topoisomerase 1(Top1) inhibitor with IC50 values of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively.
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects[1].