Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 8 |
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Ligand | BDBM21932 |
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Substrate/Competitor | Dual specificity mitogen-activated protein kinase kinase 1 |
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Meas. Tech. | Tpl2/Cot Kinase Assay |
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IC50 | 130±n/a nM |
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Citation | Green, N; Hu, Y; Janz, K; Li, HQ; Kaila, N; Guler, S; Thomason, J; Joseph-McCarthy, D; Tam, SY; Hotchandani, R; Wu, J; Huang, A; Wang, Q; Leung, L; Pelker, J; Marusic, S; Hsu, S; Telliez, JB; Hall, JP; Cuozzo, JW; Lin, 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 Chem50:4728-45 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Mitogen-activated protein kinase kinase kinase 8 |
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Name: | Mitogen-activated protein kinase kinase kinase 8 |
Synonyms: | C-COT | COT | COT proto-oncogene serine/threonine-protein kinase | Cancer Osaka thyroid oncogene | ESTF | M3K8_HUMAN | MAP3K8 | 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: | P41279 |
Residue: | 467 |
Sequence: | MEYMSTGSDNKEEIDLLIKHLNVSDVIDIMENLYASEEPAVYEPSLMTMCQDSNQNDERS
KSLLLSGQEVPWLSSVRYGTVEDLLAFANHISNTAKHFYGQRPQESGILLNMVITPQNGR
YQIDSDVLLIPWKLTYRNIGSDFIPRGAFGKVYLAQDIKTKKRMACKLIPVDQFKPSDVE
IQACFRHENIAELYGAVLWGETVHLFMEAGEGGSVLEKLESCGPMREFEIIWVTKHVLKG
LDFLHSKKVIHHDIKPSNIVFMSTKAVLVDFGLSVQMTEDVYFPKDLRGTEIYMSPEVIL
CRGHSTKADIYSLGATLIHMQTGTPPWVKRYPRSAYPSYLYIIHKQAPPLEDIADDCSPG
MRELIEASLERNPNHRPRAADLLKHEALNPPREDQPRCQSLDSALLERKRLLSRKELELP
ENIADSSCTGSTEESEMLKRQRSLYIDLGALAGYFNLVRGPPTLEYG
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BDBM21932 |
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Dual specificity mitogen-activated protein kinase kinase 1 |
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Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
Synonyms: | GST fusion of MAP kinase kinase 1 | GST-MEK1 | MAP2K1 | MEK1 | MP2K1_RABIT | PRKMK1 | 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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