top1 inhibitor 1

Top1 inhibitor 1 is a potent inhibitor of human topoisomerase I (Top1)(IC50: 29 nM).

LMP744 hydrochloride (NSC-706744 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity. 

Indotecan (LMP-400) is an effective inhibitor of topoisomerase 1(Top1) (IC50: 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively).

Compound 23, known as Top1 2-IN-1, is a dual inhibitor of Top1 2 that can be administered orally and exhibits antiproliferative effects. It induces apoptosis and cell cycle arrest in cancer cells by damaging DNA and elevating reactive oxygen species levels. Additionally, Top1 2-IN-1 demonstrates antitumor activity in vivo within xenograft models.

CBX-12 is a peptide drug conjugate (PDC) that targets tumors in an antigen-independent manner and exhibits antitumor activity. Comprising a pH-sensitive peptide (pHLIP), an auto-cleavable linker, and the topoisomerase 1 (TOP1) inhibitor Exatecan, it effectively targets cancerous cells.

IndiMitecan (LMP776) is an inhibitor of topoisomerase I (Top1) with anticancer activities [1].

Topoisomerase I inhibitor 2 (ZML-8) is a highly selective DNA topoisomerase I (Top1) inhibitor that impedes Top1 activity, causing DNA damage. It arrests the cell cycle at the G2 M phase and induces apoptosis, exhibiting anti-tumor effects [1].

(±)-Evodiamine, a quinazolinocarboline alkaloid, functions as a Top1 inhibitor and exhibits anti-inflammatory, antiobesity, and antitumor properties by effectively inhibiting the proliferation of a broad range of tumor cells through apoptosis induction [1].

DiPT-4, a dual TOP1 PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to circumvent drug resistance [1].

LMP517 (NSC 781517), an indenoisoquinoline, is a potent dual TOP1 and TOP2 inhibitor that shows better antitumor activity than its parent compound LMP744 against H82 (Small Cell Lung Cancer) xenografts, inducing TOP1 cleavage complexes (TOP1ccs) and TOP2ccs [1].