CDK9 degrader-2

CDK9 degrader-2 (compound 10) inhibits purified CDK9/cyclin T1 enzyme, with an inhibition rate of 1% at 10 nM and 54% at 100 nM; it also inhibits the proliferation of U-2932 cells, with an IC₅₀ of 45 nM^[1].
CDK9 degrader-2 (1-1000 nM; 1-24 h) induces dose- and time-dependent degradation of CDK9 in U-2932 cells, while downregulating the expression of cyclin T1, Mcl-1 and c-Myc^[1].
CDK9 degrader-2 (100 nM; 24 h) selectively degrades CDK9 in U-2932 cells, with minimal effects on CDK1, CDK2, CDK4 and CDK7^[1].
CDK9 degrader-2 (10-1000 nM; 6 h) reduces pSer2-RNAP2 levels in a dose-dependent manner in U-2932 cells, with no effect on pSer5-RNAP2 levels after 6 h of treatment; it also decreases the mRNA expression of Mcl-1 and c-Myc in U-2932 cells in a dose-dependent manner^[1].
CDK9 degrader-2 (10-1000 nM; 24 h) induces apoptosis in U-2932 cells^[1].
CDK9 degrader-2 (500 nM; 12 h) degrades CDK9 in U-2932 cells via the LC3B-dependent autophagy-lysosome pathway. This process requires simultaneous binding to both CDK9 and LC3B and is independent of the ubiquitin-proteasome system. It promotes the formation of CDK9-LC3B complexes in U-2932 cells treated with Bafilomycin A1 (HY-100558) for 12 h^[1].
CDK9 degrader-2 (100 nM; 24 h) induces LC3B-dependent degradation of CDK9 in wild-type (WT) 293T cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.