Gene and Protein Information
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

CDC2 related protein kinase 7 | cell division cycle 2-related protein kinase 7 | CRK7 | CRKR

Database Links
Alphafold	Q9NYV4 (Hs), Q14AX6 (Mm), Q3MJK5 (Rn)
BRENDA	2.7.11.22, 2.7.11.23
ChEMBL Target	CHEMBL3559692 (Hs)
Ensembl Gene	ENSG00000167258 (Hs), ENSMUSG00000003119 (Mm), ENSRNOG00000006000 (Rn), ENSRNOG00000028430 (Rn)
Entrez Gene	51755 (Hs), 69131 (Mm), 192350 (Rn)
Human Protein Atlas	ENSG00000167258 (Hs)
KEGG Enzyme	2.7.11.22, 2.7.11.23
KEGG Gene	hsa:51755 (Hs), mmu:69131 (Mm), rno:192350 (Rn)
OMIM	615514 (Hs)
Pharos	Q9NYV4 (Hs)
RefSeq Nucleotide	NM_016507 (Hs), NM_001109626 (Mm), NM_001033867 (Rn)
RefSeq Protein	NP_057591 (Hs), NP_001103096 (Mm), NP_001029039 (Rn)
UniProtKB	Q9NYV4 (Hs), Q14AX6 (Mm), Q3MJK5 (Rn)
Wikipedia	CDK12 (Hs)

Enzyme Reaction
EC Number: 2.7.11.22 EC Number: 2.7.11.23

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference CDK12 inhibitor 2 Hs Inhibition 7.3 pIC50 1 ⤷ pIC50 7.3 (IC50 5.2x10-8 M) [1] SY-5609 Hs Inhibition 5.8 pIC50 2 ⤷ pIC50 5.8 (IC50 1.702x10-6 M) [2]

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].