CDK12-IN-2

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].

Product Specifications

CAS Number

[2244987-03-7]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

CDK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cdk12-in-2.html

Purity

99.36

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(NCC1=CC=CC=C1)N([C@H]2CC[C@@H](CC2)NC3=CC=C(C=N3)C#N)C4=CC=C(C5=CN(C(C=C5)=O)C)C=C4

Molecular Formula

C32H32N6O2

Molecular Weight

532.64

Precautions

H315, H319, H320

References & Citations

[1]Masahiro Ito, et al. Discovery of 3-Benzyl-1- (trans-4- ((5-cyanopyridin-2-yl) amino) cyclohexyl) -1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. J Med Chem. 2018 Sep 13;61 (17) :7710-7728.