Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway[1].
Razoxane (ICRF 159) is an antiangiogenic topoisomerase II inhibitor, can be used for the research of renal cell carcinoma (RCC)[1].
β-Lapachone is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks[1].
DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells[1].
MC-DOXHZN hydrochloride is an albumin-binding prodrug of Doxorubicin, with acid-sensitive properties[1].
Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area[1][2].
9-Methoxycamptothecin (MCPT), isolated from Nothapodytes foetida, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer[1][2].
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research[1].
Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor[1][2][3].
Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II[1].
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase[1].
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities[1][2][3].
Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis[1].
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[1][2][3][4].
Ganoderic acid X is a lanostanoid triterpene that can be extracted from Ganoderma amboinense. Ganoderic acid X inhibits topoisomerases and induces Apoptosis of cancer cells[1].
VXc-486 is a gyrase B inhibitor, with bactericidal activity. VXc-486 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively[1].
Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
Topoisomerase inhibitor 2 (18C) is a bacterial topoisomeraseinhibitor that exhibits potent broad-spectrum activity against multidrug-resistant Gram-negative bacteria[1].
Aldoxorubicin (INNO-206) is an albumin-binding prodrug of doxorubicin, which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in in murine tumor models.
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research[1][2][3][4].
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect[1].
Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells[1][2][3].
Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity[1].
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential[1].
Rubitecan (RFS 2000), a camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells[1][2][3].
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases[1].
Nalidixic Acid-d5 is the deuterium labeled Nalidixic acid. Nalidixic acid, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria[1].