JH-XI-10-02

• CAT Number: I019416
• CAS Number: 2209085-22-1
• Molecular Formula: C₅₃H₆₉N₅O₉
• Molecular Weight: 920.14
• Purity: ≥95%

JH-XI-10-02 (CAT: I019416) is a highly potent and selective PROTAC (proteolysis-targeting chimera) CDK8 degrader. It efficiently promotes the ubiquitination and subsequent proteasomal degradation of CDK8, without affecting CDK8 mRNA levels. JH-XI-10-02 acts as a bivalent small molecule degrader by recruiting the E3 ligase CRL4Cereblon to target CDK8 for degradation. It demonstrates significant degradation of CDK8 in various cell lines, including Jurkat cells and WT Molt4 cells, but not in CRBN-null Molt4 cells. These findings highlight the potential of JH-XI-10-02 as a valuable tool for studying the biological functions of CDK8 and exploring therapeutic strategies targeting CDK8-mediated signaling pathways.

Reference

[1]. Hatcher JM, et al. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Mar 18;9(6):540-545.