top1 inhibitor 1

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

(±)-Evodiamine is an alkaloid isolated from Evodiae fructus and a topoisomerase I inhibitor. It also inhibits adipocyte differentiation and diabetes by downregulating IGF-1/HIF-1α and IL-6/STAT pathways. As an inhibitor of NF-κB activation, it suppresses invasion, promotes apoptosis, and inhibits TNF-induced Akt activation.

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.

Top1-IN-2 (Compound 1a) is an inhibitor of topoisomerase 1 (Top1). It suppresses the growth of P-gp drug-resistant tumor cells and induces apoptosis.

TOP1/TDP1-IN-1 is an inhibitor of DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) with a TDP1 IC50 of 17.8 μM. It directly inhibits the catalytic activity of TOP1 without forming a DNA-TOP1 ternary complex. This compound disrupts TDP1-mediated TOP1-induced DNA damage repair, exhibits low acute toxicity, and interferes with DNA repair pathways. It induces apoptosis, inhibits clonogenic capacity, and produces antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be utilized in research on non-small cell lung cancer, cervical cancer, and colon cancer.

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].

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].