2244987-03-7
2244987-03-7 structure
- Name: CDK12-IN-2
- Chemical Name: CDK12-IN-2
- CAS Number: 2244987-03-7
- Molecular Formula: C32H32N6O2
- Molecular Weight: 532.64
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2021-09-06 09:02:08
- Modify Date: 2024-01-10 16:22:58
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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].
| Name | CDK12-IN-2 |
|---|
| 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 |
|---|---|
| Molecular Weight | 532.64 |