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TargetInhibitor of nuclear factor kappa-B kinase subunit epsilon
LigandBDBM27468
Substrate/CompetitorI-kappa-B-alpha
Meas. Tech.IKK Kinase Inhibition Assay
IC50>15849±n/a nM
Citation Christopher, JAAvitabile, BGBamborough, PChampigny, ACCutler, GJDyos, SLGrace, KGKerns, JKKitson, JDMellor, GWMorey, JVMorse, MAO'Malley, CFPatel, CBProbst, NRumsey, WSmith, CAWilson, MJ The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. Bioorg Med Chem Lett17:3972-7 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Name:Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Synonyms:I kappa-B kinase epsilon | I-kappa-B Kinase 3 (IKK-epsilon) | I-kappa-B kinase epsilon (IKK-E) | I-kappa-B kinase epsilon (IKKE) | IKBKE | IKK-E | IKK-epsilon | IKK-i | IKKE | IKKE_HUMAN | IKKI | Inducible I kappa-B kinase | KIAA0151 | von Hippel-Lindau disease tumor suppressor/Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Type:Serine/threonine-protein kinase
Mol. Mass.:80475.98
Organism:Homo sapiens (Human)
Description:Kinase inhibitory activity was determined using recombinant human IKK-epsilon expressed in baculovirus as a FLAG-tagged fusion protein.
Residue:716
Sequence:
MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLR
KLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVV
AGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYL
HPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTE
KPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFA
ETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCV
LEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLG
AGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSV
AGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSI
QQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKY
QASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKG
AQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
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BDBM27468
I-kappa-B-alpha
Name:NF-kappa-B inhibitor alpha
Synonyms:I-kappa-B-alpha | IKBA | IKBA_HUMAN | MAD3 | NF-kappa-B inhibitor alpha | NFKBI | NFKBIA
Type:GST fusion protein
Mol. Mass.:35584.84
Organism:Homo sapiens (Human)
Description:It was produced in E. coli as GST-tagged fusion protein (Santa Cruz Biotechnology).
Residue:317
Sequence:
MFQAAERPQEWAMEGPRDGLKKERLLDDRHDSGLDSMKDEEYEQMVKELQEIRLEPQEVP
RGSEPWKQQLTEDGDSFLHLAIIHEEKALTMEVIRQVKGDLAFLNFQNNLQQTPLHLAVI
TNQPEIAEALLGAGCDPELRDFRGNTPLHLACEQGCLASVGVLTQSCTTPHLHSILKATN
YNGHTCLHLASIHGYLGIVELLVSLGADVNAQEPCNGRTALHLAVDLQNPDLVSLLLKCG
ADVNRVTYQGYSPYQLTWGRPSTRIQQQLGQLTLENLQMLPESEDEESYDTESEFTEFTE
DELPYDDCVFGGQRLTL
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