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.
Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription.
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].
CP-67804 is a quinolone derivative, is a topoisomerase II-targeted agent. CP-67804 effectively enhances DNA cleavage mediated by eukaryotic topoisomerase II. CP-67804 has potential as an antineoplastic agent[1].
Datopotamab deruxtecan (DS-1062; Dato-DXd) is a trophoblast cell surface antigen 2 (TROP2)-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan has a potent antitumor activity[1].
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].
Camptothecin-20(S)-O-propionate (Camptothecin-20-O-propionate) hydrate, the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate hydrate is a topoisomerase-Ι inhibitor[1][2].
Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC50 value of 29 nM[1].
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity[1].
Cu(II)-Elesclomol is a Cu2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces apoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity[1].
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].
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway[1][2][3][4][5][6].
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].