Cyclin-dependent kinase 9 (CDK9) plays a critical role in regulating transcriptional elongation and is essential for the expression of short-lived oncogenic and antiapoptotic mRNAs. Targeting CDK9 has emerged as a promising therapeutic strategy, particularly in hematological malignancies and MYC-driven cancers. However, its clinical application remains limited by several challenges, which may be overcome through the development of more selective and potent inhibitors.

Researchers from Shenyang Pharmaceutical University and affiliated organizations have reported the identification of a selective cyclin-dependent kinase 9 (CDK9) inhibitor, CLZX-205, being developed for the treatment of colorectal cancer.

In work conducted at China Pharmaceutical University, synthesis and optimization of a new series of cyclin-dependent kinase 9 (CDK9) inhibitors bearing a flavonoid scaffold led to the identification of compound [I] as the lead candidate, with IC50 of 6.7 nM for CDK9 and >80-fold selectivity over CDK2 and most other CDK family members.

Researchers from Biolexis Therapeutics Inc. presented the development of a potent and highly selective CDK9 inhibitor, BLX-3030, and its analogues for the treatment of N-Myc and c-Myc-driven cancers.

Researchers from Southeast University and Huanghuai University have reported the discovery of novel cyclin-dependent kinase 9 (CDK9) inhibitors as potential anticancer agents.