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cyclin dependent kinase 12

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Target not currently curated in GtoImmuPdb

Target id: 1965

Nomenclature: cyclin dependent kinase 12

Abbreviated Name: CDK12

Family: CRK7 subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1490 17q12 CDK12 cyclin dependent kinase 12
Mouse - 1484 11 61.75 cM Cdk12 cyclin-dependent kinase 12
Rat - 1484 10q31 Cdk12 cyclin-dependent kinase 12
Previous and Unofficial Names Click here for help
CDC2 related protein kinase 7 | cell division cycle 2-related protein kinase 7 | CRK7 | CRKR
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction Click here for help
EC Number: 2.7.11.22
EC Number: 2.7.11.23

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
CDK12 inhibitor 2 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.3 pIC50 1
pIC50 7.3 (IC50 5.2x10-8 M) [1]
General Comments
Mutations in CDK12 that have been found in tumours and pharmacological CDK12 inhibition sensitise cancer cells to DNA-damaging reagents and DNA-repair inhibitors. This selective CDK12 inhibitors are being investigated for potential oncology efficacy. CDK12 inhibitor 2 is a compound that is a suitable tool for studying the effects of CDK12 inhibition in RNA biology and the role of this mechanism in inducing cancer cell synthetic lethality. CDK12 inhibitor 2 selectively inhibits CDK12 and the closely related CDK13 over other C-terminal domain serine kinases [1].

References

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1. Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M et al.. (2018) 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, 61 (17): 7710-7728. [PMID:30067358]

How to cite this page

CRK7 subfamily: cyclin dependent kinase 12. Last modified on 28/08/2018. Accessed on 23/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1965.