Abstract :It is obvious that theranostic (diagnosis and treatment) of cancer is one of most urgent and important challenges in cancer therapy. Cyclometalated iridium (Ir (III)) complexes such as fac-Ir (tpy)3 1 (tpy = 2-(4-tolyl)pyridine) (Figure 1) draw an increasing attention as one of the potential imaging tools to study extra-and intracellular events, because of their significant stability and excellent photo physical properties such as high-luminescence quantum yields, the long luminescence lifetimes (~µs order), and significant Stokes shift under physiological conditions. We previously reported some examples of Ir complexes that can be functionalized as red and white color emitters, pH sensors, photosensitizers and cell death inducer of cancer cells [1-5]. Recently, we proposed artificial luminescent Ir complexe-peptide hybrids (IPHs)2 having cationic peptides that bind to anionic biomolecules on the cell membrane or cyclic peptide units that bind to death receptors (DRs) overexpressed on cancer cells, as inducers and detectors of cell death of cancer cells, typically, a human T-lymphoma Jurkat cells.