CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor ( IC 50 =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 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 IC 50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC 50 of 0.8 μM in SK-BR-3 cells. CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CDK12 52 nM (IC 50 ) CDK2 >100 μM (IC 50 ) CDK7 >10 μM (IC 50 ) CDK9 16 μM (IC 50 )
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CDK12-IN-2
CAS number：2244987-03-7(DMSO) molecular formula：C32H32N6O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2244987-03-7(DMSO) | molecular formula | C32H32N6O2 |
| molecular weight | 532.64 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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