IN6CPBD

IN6CPBD is a **pyrrolo[2,1-c][1,4]benzodiazepine (PBD)** and **indole** conjugate designed as a novel antitumor agent. It selectively induces apoptosis in cancer cells by binding to DNA and forming an adduct at the N2 position of guanine. The compound demonstrates potent tumor-suppressive effects and improved safety compared to its parent compound (DC-81), particularly in mouse models of melanoma and various cancer cell lines. IN6CPBD suppresses tumor growth and metastasis and elicits robust apoptosis of malignant cells with minimal cardiotoxicity and liver toxicity. Mechanistically, it displays selective inhibition and degradation of the NF-κB subunit RelA/p65, disrupting NF-κB signal transduction which is key for tumor proliferation and resistance, through both DNA binding and proteasome-mediated degradation pathways. Its specificity for tumor cells over normal cells suggests a favorable therapeutic index[1][2][3].

Other names

Pyrrolo[2,1-c][1,4]benzodiazepine-indole conjugate