CB12

CB12 is a synthetic derivative of the natural product celastrol, modified at the carboxyl group to enhance its anti-tumor activity. It functions as a molecular glue that facilitates the recruitment of the E3 ubiquitin ligase UBE3A to steroid receptors, specifically the androgen receptor (AR), its variant AR-v7, and the glucocorticoid receptor (GR). This recruitment leads to the ubiquitination and subsequent proteasomal degradation of these receptors. CB12 has demonstrated potent inhibitory effects on prostate cancer cell proliferation and tumor growth in preclinical models, showing superior efficacy compared to the AR antagonist enzalutamide, particularly in models of castration-resistant prostate cancer (CRPC).

Other names

celastrol derivative CB12