topoisomerase IIα

Topoisomerase IIα-IN-9 ,with CAS No. 16346-97-7, is a fragment molecule that serves as an important scaffold for molecular linking, expansion, and modification. Topoisomerase IIα-IN-9 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.

TopoisomeraseIIα-IN-11 (Compound 16h) is a potent inhibitor of Topoisomerase IIα (TopoisomeraseIIα). It demonstrates significant inhibitory effects on melanoma A2058 cell lines with an IC50 of 3-6 μM. TopoisomeraseIIα-IN-11 holds potential for cancer research, particularly in the study of melanoma.

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].

Topoisomerase II inhibitor 13 inhibits topoisomerase II (Topo II) that shows strong anti-proliferation activity against HL-60/MX2 cancer cells derived from HL-60 against Topo II toxicity.

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative acting as a Type II DNA topoisomerase (topo II) inhibitor. It specifically targets topo IIα/β subtypes, with IC50 values of 0.17 μM for topo IIα and 0.23 μM for topo IIβ, causing significant DNA damage and inducing apoptosis by triggering the loss of mitochondrial membrane potential [1].

Topoisomerase II inhibitor 7, a potent inhibitor of the topoisomerase II alpha subtype, exhibits an IC50 of 3.19 μM. It effectively induces cell cycle arrest and apoptosis.

TopoisomeraseI/II inhibitor 5 (compound 1) stabilizes G4 structures through binding and concurrently inhibits the relaxation activities of TopoI and II.

TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.

TopoisomeraseII Inhibitor 20 TFA is a potent inhibitor of topoisomerase II with an IC50 of 0.98 µM. It can induce cell apoptosis and exhibits broad-spectrum anticancer activity.

Compound 5h (Topoisomerase I/II inhibitor 7) is a Topoisomerase I/II inhibitor.

TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.

TopoisomeraseII/EGFR-IN-1 is a dual inhibitor of topoisomerase II and EGFR, exhibiting strong cytotoxic activity against the MCF-7, A549, and HCT-116 cell lines. It also demonstrates significant apoptotic activity, making it useful for cancer research.

TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.

Topoisomerase II inhibitor 19 (compound 5h) is a DNA intercalator and a topoisomerase II inhibitor with an IC50 of 0.34 μM. It induces damage in ctDNA.

TopoisomeraseII inhibitor 20 (Compound 3e) is a potent inhibitor of Topoisomerase II, with an IC50 of 0.98 µM. It can induce apoptosis and possesses broad-spectrum anticancer activity.

TopoisomeraseII inhibitor 23 is a potent inhibitor of topoisomerase II (topoisomeraseII) with an IC50 value of 0.94 μM. Compared to doxorubicin (IC50 of 3.08 μM), it exhibits high selectivity and superior cytotoxic effects in MCF-7, HepG2, and HCT116 cells. This compound induces cell cycle arrest at the G1 phase, leading to the inhibition of cell proliferation. It also promotes apoptosis (apoptosis) by upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-2.

TopoisomeraseI/II-IN-1 is a dual inhibitor of Topoisomerase I and II. It induces G2/M cell cycle arrest and apoptosis (apoptosis) in cancer cells by increasing the levels of p53, p21, Bax mRNA, and caspase-3 proteins, as well as the Bax/Bcl-2 ratio, while decreasing Bcl-2 levels. This compound is useful for research on various cancers such as melanoma, renal cancer, colorectal cancer, and breast cancer.

Topoisomerase II inhibitor 8 (compound 22) is a potent inhibitor of topoisomerase II (IC50 = 0.52 μM) [1] and exhibits strong anti-proliferative activities, arresting the cell cycle at the G2/M phase.

Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective topoisomerase II inhibitor that blocks the CCRF-CEM cell cycle in the G2 phase and induces DNA double-strand breaks (DSB). It exhibits antiproliferative activity on various tumor cell lines and has potential for cancer research [1].