GT-02897

GT-02897 is a selective, small-molecule proteolysis-targeting chimera (PROTAC) designed to induce the degradation of cyclin-dependent kinase 9 (CDK9). Developed by Gluetacs Therapeutics in collaboration with researchers at Shanghai Jiao Tong University and Xinhua Hospital, the compound targets the P-TEFb complex component to disrupt the transcriptional elongation of short-lived oncogenic survival genes such as MYC, MCL-1, and MDM2. Beyond its role in transcriptional regulation, GT-02897 has been shown to relieve CDK9-mediated degradation of the retinoic acid receptor alpha (RARα) by preventing the recruitment of the E3 ligase HUWE1. This dual mechanism sensitizes malignant cells to all-trans retinoic acid (ATRA) and exhibits synergistic activity with BCL-2 inhibitors like venetoclax and sonrotoclax. GT-02897 is currently in preclinical development for the treatment of cutaneous T-cell lymphoma (CTCL) and multiple myeloma.