CDK-IN-12

CDK-IN-12 (Example 20), a CDK inhibitor, effectively inhibits CDK4 6, demonstrating IC50 values below 20 nM [1].

CDK12-IN-3 is a selective and potent CDK12 inhibitor with anti-tumor activity, which can be used to study malignant tumors.

CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.

CDK9-IN-12 is a highly selective CDK9 inhibitor, which is commonly used in leukemia research to regulate oncogene expression, inhibit oncogenic proliferation, and induce apoptosis by targeting CDK9-dependent transcription processes.

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).

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2 Cyclin E (IC50 >20 μM) and CDK9 Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

CDK7 12-IN-1 is a selective inhibitor of CDK7 (IC50: 3 nM) and CDK12 (IC50: 277 nM) and effectively inhibits tumor growth.