Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase 8 |
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Ligand | BDBM29912 |
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Substrate/Competitor | Dual specificity mitogen-activated protein kinase kinase 1 |
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Meas. Tech. | Tpl2/Cot ELISA Assay |
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pH | 7.2±n/a |
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Temperature | 303.15±n/a K |
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IC50 | 3±n/a nM |
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Citation | Wu, J; Green, N; Hotchandani, R; Hu, Y; Condon, J; Huang, A; Kaila, N; Li, HQ; Guler, S; Li, W; Tam, SY; Wang, Q; Pelker, J; Marusic, S; Hsu, S; Perry Hall, J; Telliez, JB; Cui, J; Lin, LL Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood. Bioorg Med Chem Lett19:3485-8 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, 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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BDBM29912 |
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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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