CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).

CDK-IN-9 (compound 24) is a potent inhibitor of CDK. CDK-IN-9 is also a molecular gel that induces interaction between CDK12 and DDB1 and is able to act on CDK2/E (IC50: 4 nM). CDK-IN-9 can be used to dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).