Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	-	419	19p13.3-p13.2	MAP2K7	mitogen-activated protein kinase kinase 7
Mouse	-	419	8 A1.1	Map2k7	mitogen-activated protein kinase kinase 7
Rat	-	419	12 p12	Map2k7	mitogen activated protein kinase kinase 7
Gene and Protein Information Comments
Multiple alternatively spliced transcript variants encoding distinct isoforms have been found, but only the transcript variant generating the 419 amino acid protein has been supported and defined. Isoform B is postulated to contain a 43 amino acid insertion, translating to a 462 amino acid protein.

Previous and Unofficial Names

c-Jun N-terminal kinase kinase 2 | dual specificity mitogen-activated protein kinase kinase 7 | JNK kinase 2 | JNKK2 | MAP kinase kinase 7 | MKK7 | PRKMK7 | SAPKK4 | sek2 | SKK4 | Stress-activated protein kinase kinase 4

Database Links
BRENDA	2.7.12.2
ChEMBL Target	CHEMBL3530 (Hs)
Ensembl Gene	ENSG00000076984 (Hs), ENSMUSG00000002948 (Mm), ENSRNOG00000001047 (Rn)
Entrez Gene	5609 (Hs), 26400 (Mm), 363855 (Rn)
Human Protein Atlas	ENSG00000076984 (Hs)
KEGG Enzyme	2.7.12.2
KEGG Gene	hsa:5609 (Hs), mmu:26400 (Mm), rno:363855 (Rn)
OMIM	603014 (Hs)
RefSeq Nucleotide	NM_145185 (Hs), NM_011944 (Mm), NM_001025425 (Rn)
RefSeq Protein	NP_660186 (Hs), NP_036074 (Mm), NP_001020596 (Rn)
UniProtKB	O14733 (Hs), Q8CE90 (Mm), Q4KSH7 (Rn)
Wikipedia	MAP2K7 (Hs)

Enzyme Reaction
EC Number: 2.7.12.2

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

Inhibitors
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Ligand Sp. Action Value Parameter Reference compound 11 [PMID: 26431428] Hs Inhibition 5.3 pIC50 3 ⤷ pIC50 5.3 (IC50 5x10-6 M) [3]

Allosteric Modulators
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Ligand Sp. Action Value Parameter Reference cobimetinib Hs Negative <5.0 pIC50 4 ⤷ pIC50 <5.0 (IC50 >1x10-5 M) [4]

DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 1,5
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Target used in screen: MKK7
Ligand Sp. Type Action Value Parameter AST-487 Hs Inhibitor Inhibition 7.6 pKd staurosporine Hs Inhibitor Inhibition 7.5 pKd lestaurtinib Hs Inhibitor Inhibition 7.1 pKd canertinib Hs Inhibitor Inhibition 7.0 pKd neratinib Hs Inhibitor Inhibition 6.3 pKd SB203580 Hs Inhibitor Inhibition <5.5 pKd ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd erlotinib Hs Inhibitor Inhibition <5.5 pKd GSK690693 Hs Inhibitor Inhibition <5.5 pKd masitinib Hs Inhibitor Inhibition <5.5 pKd
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EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: 2...
Key to terms and symbols		Click column headers to sort
Target used in screen: MKK7β/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM K-252a Hs Inhibitor Inhibition 7.0 0.0 JNK inhibitor VIII Hs Inhibitor Inhibition 11.0 4.0 staurosporine Hs Inhibitor Inhibition 11.0 1.5 isogranulatimide Hs Inhibitor Inhibition 42.0 27.0 PKR inhibitor Hs Inhibitor Inhibition 43.0 12.0 Gö 6976 Hs Inhibitor Inhibition 52.0 34.0 indirubin-3'-monoxime Hs Inhibitor Inhibition 52.0 7.0 indirubin derivative E804 Hs Inhibitor Inhibition 54.0 5.0 Cdk2 inhibitor IV Hs Inhibitor Inhibition 56.0 16.0 SP600125 Hs Inhibitor Inhibition 58.0 6.0
Displaying the top 10 most potent ligands  View all ligands in screen »