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Lapcin is a potent dual topoisomerase I/II inhibitor with nM to pM IC50s against diverse cancer cell lines (Colon cancer HT29 cell IC50=0.516 nM);
Lapcin showed weak activity against DNA gyrase (IC50>20.5 uM).
While only weakly active against DNA gyrase, lapcin was a potent of inhibitor of both DNA relaxation by topoisomerase I (IC50=2.17 uM) and DNA decatenation by topoisomerase II (IC50=7.53uM), 14 times more potent than the alkaloid camptothecin.
Lapcin was more potent than the topoisomerase II inhibitor etoposide against all of the cell lines we tested, with the exception of the lung cancer cell NCI-H226, against which it was essentially equipotent.
Cell lines expressing wild-type p53 (HCT116, H226, MCF7) tended to show higher IC50s than p53 reduced cell lines (NCI-H1299, HT29, Colo205, Hela).
Eleutherin ((+)-Eleutherin) is a pyranonaphthoquinones that is isolated from the bulb of Eleutherine americana and a potent catalytic inhibitor of Topoisomerase II. It exhibits potent anti-cancer activity and protects human umbilical vein endothelial cells (HUVECs) from injury in vitro.
ABBV-969 Payload is an agent-linker conjugate with a potent inhibitor of topoisomerase I and a linker designed for use in the antibody-drug conjugate (ADC) ABBV-969. It can be used in non-small cell lung cancer research.
β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers.
OSUAB-0284 is a bacterial topoisomerase inhibitor. OSUAB-0284 has significant anti-staphylococcal activity, especially against methicillin-resistant Staphylococcus aureus (MRSA). OSUAB-0284 exerts its antibacterial effect by inhibiting bacterial topoisomerase. OSUAB-0284 can be used to study infections caused by drug-resistant bacteria such as MRSA.
Mal-Exatecan is a Mal (Maleimide) modified Exatecan. Rilpivirine is an effective and selective diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). It exhibits potent antiviral activity against both wild-type HIV (EC50 = 0.4 nM) and mutant strains (EC50 = 0.1-2.0 nM).
GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile.
AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents.
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