1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-2

CDK12-IN-2 

Cat. No.: HY-112626
Handling Instructions

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.

For research use only. We do not sell to patients.

CDK12-IN-2 Chemical Structure

CDK12-IN-2 Chemical Structure

CAS No. : 2244987-03-7

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

532.64

Formula

C₃₂H₃₂N₆O₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Product Name:
CDK12-IN-2
Cat. No.:
HY-112626
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