Targeting regulatory enzymes is an important aspect of chemical biology. The approach involves acquiring target enzymes through heterologous expression, studying their properties, and ultimately applying them in practical settings. Microcystinase A (MlrA) was identified and successfully prepared and characterized as a target enzyme. The study analyzed both the purity of the enzyme and its resulting effects, examining how different substrate concentrations, temperature, pH, and metal ions affected MlrA’s activity in microcystins (MCs) degradation. Through experimentation and exploration, students can learn to prepare and analyze target proteins, design experiments to explore enzyme activity under different conditions, and use key instruments, which improves their problem-solving skills, their ability to apply chemical biology knowledge, and their scientific inquiry and social responsibility. In the process of experimental teaching, students were guided to think about the value and significance of scientific research to society, realize the importance of scientific ethics and social responsibility, and understand the social responsibility and mission of scientific researchers, which cunltivate their senses of scientific inquiry and social responsibility.