CDK-IN-9 

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC₅₀ values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II^[1].

CDK-IN-9 (compound 24) (0.005, 0.05, 0.5, or 5 μM; 2 h) potently decreases the level of cyclin K in MINO cells at 5 nM, and makes cyclin K disappear completely at 50 nM^[1].
CDK-IN-9 makes siRNA silencing of DDB1 effectively stabilizes cyclin K at the protein level in treated MINO cells^[1].
CDK-IN-9 (2.5-40 nM; 24 h) activates caspases 3/7/9 and decreases anti-apoptotic proteins Mcl-1 and XIAP in MINO cells^[1].

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

CDK-IN-9 (0.1-10 mg/kg; IP, single dosage) causes the decrease in cyclin K and CDK12 levels^[1].

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

420.53

C₂₁H₂₄N₈S

3031561-92-6

NCCSC1=NC2=C(NN=C2C(NCC3=CC=C(C=C3)N4C=CC=N4)=N1)C5CCC5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jorda R, et al. 3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders. J Med Chem. 2022 Jul 14;65(13):8881-8896.  [Content Brief]