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TargetMitogen-activated protein kinase kinase kinase 8
LigandBDBM29903
Substrate/CompetitorDual specificity mitogen-activated protein kinase kinase 1
Meas. Tech.Tpl2/Cot ELISA Assay
pH7.2±n/a
Temperature303.15±n/a K
IC50 10±n/a nM
Citation Wu, JGreen, NHotchandani, RHu, YCondon, JHuang, AKaila, NLi, HQGuler, SLi, WTam, SYWang, QPelker, JMarusic, SHsu, SPerry Hall, JTelliez, JBCui, JLin, 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
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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BDBM29903
NameBDBM29903
Synonyms:substituted 6-aminoquinoline-3-carbonitrile, 14
TypeSmall organic molecule
Emp. Form.C25H17Cl2FN8
Mol. Mass.519.36
SMILESFc1ccc(Nc2c(cnc3c(Cl)cc(NCc4cn(Cc5cccnc5)nn4)cc23)C#N)cc1Cl
Structure
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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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