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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM21908
Substrate/CompetitorDual specificity mitogen-activated protein kinase kinase 1
Meas. Tech.Tpl2/Cot Kinase Assay
pH7.2±n/a
Temperature303.15±n/a K
IC50 830±n/a nM
Citation Green NHu YJanz KLi HQKaila NGuler SThomason JJoseph-McCarthy DTam SYHotchandani RWu JHuang AWang QLeung LPelker JMarusic SHsu STelliez JBHall JPCuozzo JWLin LL Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles. J Med Chem 50:4728-45 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Mitogen-activated protein kinase kinase kinase 8
Name:Mitogen-activated protein kinase kinase kinase 8
Synonyms:C-COT | COT proto-oncogene serine/threonine-protein kinase | Cancer Osaka thyroid oncogene | Mitogen-activated protein kinase kinase kinase 8 | Tpl-2 | Tumor Progression Loci-2 Kinase (COT) | Tumor progression locus 2
Type:Serine/threonine-protein kinase
Mol. Mass.:52916.89
Organism:Homo sapiens (Human)
Description:n/a
Residue:467
Sequence:
MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
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BDBM21908
Dual specificity mitogen-activated protein kinase kinase 1
Name:Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:GST fusion of MAP kinase kinase 1 | GST-MEK1 | glutathione S-transferase-MAP kinase kinase 1
Type:Other Protein Type
Mol. Mass.:43453
Organism:Oryctolagus cuniculus (rabbit)
Description:Rabbit MEK1 was purchased from Millipore.
Residue:393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSAVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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