CDK12-IN-2 structure
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Common Name | CDK12-IN-2 | ||
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CAS Number | 2244987-03-7 | Molecular Weight | 532.64 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C32H32N6O2 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of CDK12-IN-2CDK12-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]. |
Name | CDK12-IN-2 |
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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]. |
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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 |
Molecular Formula | C32H32N6O2 |
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Molecular Weight | 532.64 |