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29 Results for "
Topoisomerase IIα
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "Topoisomerase IIα" in MCE Product Catalog:
3
3 Cited Publications
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PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs) .
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ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
Cat. No.: HY-151453
CAS No.: 2860554-26-1
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Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
Cat. No.: HY-12888
CAS No.: 907543-25-3
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AZD5099 is an orally effective pyrrole amide inhibitor and antibacterial agent. AZD5099 shows over 10000-fold higher selectivity for bacterial type II topoisomerases than for human topoisomerase IIα, with a IC50 value of 0.032 μmol/L against Staphylococcus aureus GyrB, a IC50 of 0.760 μmol/L against Escherichia coli GyrB, a IC50 of 73 nM against Escherichia coli ParE, a Kd of 83.8 nmol/L for Staphylococcus aureus GyrB, and a IC50 of >50 μM against human topoisomerase IIα. AZD5099 inhibits rat Mrp2 ATPase activity, competitively binds to the ATP-binding site of bacterial type II topoisomerases, blocks enzyme activity, reduces bacterial DNA and RNA synthesis, disrupts DNA replication and transcription processes, and induces mitochondrial toxicity. AZD5099 exhibits activity against Gram-positive bacteria, fastidious Gram-negative bacteria and drug-resistant strains, reduces bacterial loads in mouse infection models, and has a low spontaneous resistance frequency. AZD5099 can be used in studies related to infections caused by Gram-positive bacteria and fastidious Gram-negative bacteria, methicillin-resistant Staphylococcus aureus infections, Streptococcus pneumoniae pulmonary infections, as well as Staphylococcus aureus and Escherichia coli infections .
Cat. No.: HY-174837
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Topoisomerase IIα-IN-11 (Compound 16h) is a potent Topoisomerase IIα inhibitor. Topoisomerase IIα-IN-11 shows significant inhibition on melanoma A2058 cell lines (IC50 3-6 μM). Topoisomerase IIα-IN-11 is promising for research of cancers (especially melanoma) .
Cat. No.: HY-170557
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Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment .
Cat. No.: HY-146020
CAS No.: 2407521-87-1
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Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .
Cat. No.: HY-147801
CAS No.: 2538528-11-7
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Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
Cat. No.: HY-152473
CAS No.: 3042869-61-1
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Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism .
Cat. No.: HY-152187
CAS No.: 3037545-23-3
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Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629) .
Cat. No.: HY-152479
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Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .
Cat. No.: HY-146021
CAS No.: 2407521-90-6
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Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
Cat. No.: HY-18626
CAS No.: 208237-49-4
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NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
Cat. No.: HY-143279
CAS No.: 99140-25-7
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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 .
Cat. No.: HY-117543
CAS No.: 160554-87-0
Synonyms: AMP-53; 6-Ethoxyazonafide
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Ethonafide (AMP-53) is an anthracene-containing derivative of Amonafide that belongs to the Azonafide series of anticancer agents. Ethonafide (AMP-53) inhibits topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIα and β .
Cat. No.: HY-W031307
CAS No.: 1251578-67-2
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Topoisomerase IIα-IN-8 (compound 15) is a weak human DNA topoisomerase IIa (htIIa) inhibitor, with an IC50 of 462 ± 38.0 μM .
Cat. No.: HY-W178011
CAS No.: 16346-97-7
Synonyms: 4,4'-Sulfonylbis(2-methylphenol)
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Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that has a moderate inhibitory effect on DNA topoisomerase Topoisomerase II (IC50: 571 μM). Topoisomerase IIα-IN-9 also exhibits a certain cell growth inhibitory effect, with IC50s of 117 μM and 218 μM for K562 and CHO, respectively .
Cat. No.: HY-126333
CAS No.: 2375613-31-1
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Topoisomerase II inhibitor 1 (compound 89) is a highly efficient and selective topoisomerase IIα inhibitor .
Cat. No.: HY-146163
CAS No.: 2697171-03-0
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Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis .
Cat. No.: HY-180509
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Topoisomerase I/IIα-IN-1 (Compound 20i) is a Topoisomerase I/IIα inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has relatively poor anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
