||MSC2530818 is a Potent, Selective, and Orally Bioavailable CDK8 Inhibitor with CDK8 IC50 = 2.6 nM; Human PK prediction: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%.
||CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with potential antineoplastic and chemoprotective activities.
||THZ531 is a covalent CDK12 and CDK13 covalent inhibitor. Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription.
||THZ2, an analog of THZ1, with the potential to treat Triple-negative breast cancer (TNBC), it is a potent and selective CDK7 inhibitor which overcomes the instability of THZ1 in vivo. IC50: CDK7= 13.9 nM; TNBC cells= 10 nM