topoisomerase IIα

Compound EN300-20599, with CAS No. 16346-97-7, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Compound EN300-20599 provides a structural basis and research tool for the design and screening of novel drug candidates, and is commonly used in drug discovery, drug synthesis, and related research.

TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg/kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg/mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, selectively inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It induces apoptosis and arrests the cell cycle in HepG2 cells, demonstrating strong antitumor effects against various human cancer cell lines, thereby highlighting its significance for cancer research [1].

Topoisomerase IIα-IN-1 (compound 2) is a potent TopoIIα inhibitor and DNA-binding ligand, exhibiting significant anti-proliferative effects on human cancer cell lines.

Topoisomerase IIα-IN-2 (compound 5) is a potent inhibitor of the topoisomerase TopoIIα and a DNA-binding ligand. It exhibits high anti-proliferative activity in human cancer cell lines, arrests the cell cycle in the G2/M phase, and significantly induces DNA damage.

Topoisomerase IIα-IN-3 is a DNA-inserting topoisomerase-Iiα inhibitor that blocks the cell cycle in G0/G1 phase and induces apoptosis.

Topoisomerase IIα-IN-8 (compound 15) serves as a modest inhibitor of human DNA topoisomerase IIα (htIIα), exhibiting an inhibitory concentration (IC50) of 462 ± 38.0 μM [1].

Banoxantrone dihydrochloride (AQ4N dihydrochloride) is a novel hypoxic cytotoxin that selectively kills hypoxic cells through an iNOS-dependent mechanism.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

Daniquidone (Batracylin) is a potent dual inhibitor of DNA topoisomerase I and DNA topoisomerase II with cytotoxic and antiproliferative activity that induces DNA fragmentation for the study of neoplasms, immune disorders, and lymphatic disorders.

Aldoxorubicin has effective antitumor activities in various cancer cell lines and in murine tumor models. Aldoxorubicin is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitors).

Zabofloxacin is a potent and seletive bacterial type II and IV topoisomerases inhibitor, and has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.

Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

Intoplicine is an inhibitor of DNA topoisomerase I and II.

Phenoxodiol (Idronoxil) activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.

Pyronaridine tetraphosphate is an orally active, mannitol-containing inhibitor of DNA topoisomerase 2 and erythrocyte cytokine with antimalarial and antitumour activity.Pyronaridine tetraphosphate treats P. falciparum and Echinococcus granulosus infections. Pyronaridine tetraphosphate treats P. falciparum and Echinococcus granulosus infections and attenuates Ebola virus transmission.

Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibitor with anticancer and antioxidant activities.Topoisomerase II inhibitor 14 induces apoptosis and blocks the cell cycle in S phase.Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO. Topoisomerase II inhibitor 14 reduces the amount of GSH, MDA and NO.

Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme.

Proscillaridin A is a natural product.It is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.

3α, 27-Dihydroxylupen-20(29)-en-28-oic acid methyl ester is a topoisomerase II inhibitor.

AuL1 is a topoisomerase IIα (Top II) inhibitor with DNA intercalating properties. It exhibits cytotoxic effects on tumor cells, making it a potential subject for anticancer agent research.

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, utilized in cancer research.