Reaction Details |
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Target | Inhibitor of nuclear factor kappa-B kinase subunit beta |
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Ligand | BDBM29427 |
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Substrate/Competitor | I-kappa-B-alpha |
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Meas. Tech. | IKK Kinase Inhibition Assay |
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IC50 | 2512±n/a nM |
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Citation | Christopher, JA; Bamborough, P; Alder, C; Campbell, A; Cutler, GJ; Down, K; Hamadi, AM; Jolly, AM; Kerns, JK; Lucas, FS; Mellor, GW; Miller, DD; Morse, MA; Pancholi, KD; Rumsey, W; Solanke, YE; Williamson, R Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta). J Med Chem52:3098-102 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Inhibitor of nuclear factor kappa-B kinase subunit beta |
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Name: | Inhibitor of nuclear factor kappa-B kinase subunit beta |
Synonyms: | I-kappa-B Kinase 2 (IKK-beta) | I-kappa-B kinase 2 | I-kappa-B-kinase beta | I-kappa-B-kinase beta (IKKB) | IKBKB | IKK-B | IKK-beta | IKK2 | IKK2/IKK1 | IKKB | IKKB_HUMAN | Inhibitor of NF-kappa-B kinase alpha/beta | Inhibitor of nuclear factor kappa B kinase beta subunit | NFKBIKB | Nuclear factor NF-kappa-B inhibitor kinase beta |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 86554.39 |
Organism: | Homo sapiens (Human) |
Description: | GST-tagged IKK-2 was expressed in High Five cells and purified. |
Residue: | 756 |
Sequence: | MSWSPSLTTQTCGAWEMKERLGTGGFGNVIRWHNQETGEQIAIKQCRQELSPRNRERWCL
EIQIMRRLTHPNVVAARDVPEGMQNLAPNDLPLLAMEYCQGGDLRKYLNQFENCCGLREG
AILTLLSDIASALRYLHENRIIHRDLKPENIVLQQGEQRLIHKIIDLGYAKELDQGSLCT
SFVGTLQYLAPELLEQQKYTVTVDYWSFGTLAFECITGFRPFLPNWQPVQWHSKVRQKSE
VDIVVSEDLNGTVKFSSSLPYPNNLNSVLAERLEKWLQLMLMWHPRQRGTDPTYGPNGCF
KALDDILNLKLVHILNMVTGTIHTYPVTEDESLQSLKARIQQDTGIPEEDQELLQEAGLA
LIPDKPATQCISDGKLNEGHTLDMDLVFLFDNSKITYETQISPRPQPESVSCILQEPKRN
LAFFQLRKVWGQVWHSIQTLKEDCNRLQQGQRAAMMNLLRNNSCLSKMKNSMASMSQQLK
AKLDFFKTSIQIDLEKYSEQTEFGITSDKLLLAWREMEQAVELCGRENEVKLLVERMMAL
QTDIVDLQRSPMGRKQGGTLDDLEEQARELYRRLREKPRDQRTEGDSQEMVRLLLQAIQS
FEKKVRVIYTQLSKTVVCKQKALELLPKVEEVVSLMNEDEKTVVRLQEKRQKELWNLLKI
ACSKVRGPVSGSPDSMNASRLSQPGQLMSQPSTASNSLPEPAKKSEELVAEAHNLCTLLE
NAIQDTVREQDQSFTALDWSWLQTEEEEHSCLEQAS
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BDBM29427 |
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I-kappa-B-alpha |
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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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