As such, we designed and synthesized herein the first H2O2-responsive ERβ-targeted probes, which with DCM-OH form the skeleton of both the fluorophores and ERβ ligand, with borate esters as the H2O2-responsive group, thus trying to develop H2O2-triggered ERβ probes for prostate cancer imaging. Here, ESR2 is linked to prostate carcinoma.