Abstract: Gliomas, especially malignant gliomas, are the most common primary brain tumors associated with high recurrence rate and significant mortality. The combination of surgery and radio- chemotherapy is the best treatment for them nowadays. However, due to their biological characteristics of invasive growth, they do not respond well to traditional therapy. How to target the tumor in situ, and inhibit tumor cell proliferation and invasion is the key for study. In recent years, many studies have demonstrated that Buthus martensii Karsch chlorotoxin(BmK CT), an important chlorotoxin-like peptide, specifically inhibited glioma cells growth and metastasis as a blocker of the chloride ion channel and matrix metallopro-teinase-2(MMP-2). The bioconjugates of BmK CT with other molecules have played an increasing role in targeted imaging and treatment of gliomas. In this review, its source, chemical structure and mechanisms will be provided. Besides, advantages and challenges in the use of BmK CT as a specific agent for imaging and theranostic applications in gliomas will be addressed.