CDK12-IN-2
Names
[ CAS No. ]:
2244987-03-7
[ Name ]:
CDK12-IN-2
Biological Activity
[Description]:
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12[1].
[Related Catalog]:
[Target]
CDK12:52 nM (IC50)
CDK2:>100 μM (IC50)
CDK7:>10 μM (IC50)
CDK9:16 μM (IC50)
[In Vitro]
CDK12-IN-2 inhibits the phosphorylation of the CTD Ser2 in SK-BR-3 cells at low submicromolar concentrations, it inhibits C-terminal domain ser2 phosphorylation with an IC50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC50 of 0.8 μM in SK-BR-3 cells[1]. CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC50 value for CDK12-IN-2 are 0.0078 μM, 0.042 μM, 0.057 μM,and 0.059 μM, for 0h, 1h, 2h and 5h respectively[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C32H32N6O2
[ Molecular Weight ]:
532.64