Abstract : A nano-regulator induces triple homeostasis disruption of calcium ion/nitric oxide/energy metabolism for synergetic cancer therapy. Abstract : Inducing homeostasis disruption in cancer cells will cause severe cytotoxicity and apoptosis for cancer therapy. However, comprehensive intracellular active homeostatic mechanisms make it still a daunting challenge. Reported herein is a biomimetic nano-regulator for mutually reinforcing Ca 2+ /NO/energy metabolism triple homeostasis disruption via cascade reactions.