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Inhibitor of nuclear factor kappa-B kinase subunit beta

An inhibitor of nuclear factor kappa-B kinase subunit beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:O14920]

Synonyms

I-kappa-B-kinase beta;
IKK-B;
IKK-beta;
IkBKB;
EC 2.7.11.10;
I-kappa-B kinase 2;
IKK2;
Nuclear factor NF-kappa-B inhibitor kinase beta;
NFKBIKB;
Serine/threonine protein kinase IKBKB;
2.7.11.1

Research

Bioassay Publications (67)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's33 (49.25)29.6817
2010's32 (47.76)24.3611
2020's2 (2.99)2.80

Compounds (108)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
7,8-dihydroxyflavoneHomo sapiens (human)IC509.820011
aurintricarboxylic acidHomo sapiens (human)IC505.400011
7-azaindoleHomo sapiens (human)IC50648.978512
staurosporineHomo sapiens (human)IC500.556199
birb 796Homo sapiens (human)IC5025.000022
ertiprotafibHomo sapiens (human)IC500.400011
sc 514Homo sapiens (human)IC507.380045
dasatinibHomo sapiens (human)IC5010.000011
imd 0354Homo sapiens (human)IC5050.109022
diosminHomo sapiens (human)IC503.890011
wedelolactoneHomo sapiens (human)IC5010.000011
ellagic acidHomo sapiens (human)IC501.980011
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-oneHomo sapiens (human)IC500.300022
a 770041Homo sapiens (human)IC5025.000011
[4-[[4-(1-benzothiophen-2-yl)-2-pyrimidinyl]amino]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanoneHomo sapiens (human)IC500.90501010
bms345541Homo sapiens (human)IC501.000078
bms345541Homo sapiens (human)Ki0.300011
spc-839Homo sapiens (human)IC500.053855
spc-839Homo sapiens (human)Ki0.020011
gambogic acidHomo sapiens (human)IC503.070011
3,5-bis(2-fluorobenzylidene)piperidin-4-oneHomo sapiens (human)IC5072.000011
2-((aminocarbonyl)amino)-5-(4-fluorophenyl)-3-thiophenecarboxamideHomo sapiens (human)IC500.018944
bms345541Homo sapiens (human)IC501.296044
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)IC500.255022
ps1145Homo sapiens (human)IC500.164655
tak-715Homo sapiens (human)IC5010.000011
danusertibHomo sapiens (human)IC5010.000011
N-[5-[[5-[(4-acetyl-1-piperazinyl)-oxomethyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamideHomo sapiens (human)IC5050.000011
tak 285Homo sapiens (human)IC5010.000011
5-(5,6-dimethoxy-1-benzimidazolyl)-3-[(2-methylsulfonylphenyl)methoxy]-2-thiophenecarbonitrileHomo sapiens (human)IC5012.687235
pha 767491Homo sapiens (human)IC5010.000022
gsk 269962aHomo sapiens (human)IC5010.000011
sb 772077-bHomo sapiens (human)IC5010.000011
pha 848125Homo sapiens (human)IC5010.000011
pha 408Homo sapiens (human)IC500.342232
bms 777607Homo sapiens (human)IC502.000011
entrectinibHomo sapiens (human)IC5010.000011
pha 793887Homo sapiens (human)IC5010.000011
tak-632Homo sapiens (human)IC503.700011
nms p937Homo sapiens (human)IC5010.000011
nms-p118Homo sapiens (human)IC5010.000011
lfm a13Homo sapiens (human)IC50500.000011
urmc-099Homo sapiens (human)IC500.257011
bay 65-1942Homo sapiens (human)Ki0.002011
nms-e973Homo sapiens (human)IC500.010011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
imatinibHomo sapiens (human)Kd10.000011
staurosporineHomo sapiens (human)Kd0.031011
gefitinibHomo sapiens (human)Kd10.000011
lestaurtinibHomo sapiens (human)Kd0.012022
vatalanibHomo sapiens (human)Kd10.000011
ruboxistaurinHomo sapiens (human)Kd10.000011
canertinibHomo sapiens (human)Kd10.000011
birb 796Homo sapiens (human)Kd10.000011
sb 203580Homo sapiens (human)Kd10.000011
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd10.000011
lapatinibHomo sapiens (human)Kd10.000011
sorafenibHomo sapiens (human)Kd10.000022
pd 173955Homo sapiens (human)Kd10.000011
s 1033Homo sapiens (human)Kd10.000011
bms 387032Homo sapiens (human)Kd10.000011
tandutinibHomo sapiens (human)Kd10.000022
vx-745Homo sapiens (human)Kd10.000011
dasatinibHomo sapiens (human)Kd10.000011
zd 6474Homo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd10.000011
bosutinibHomo sapiens (human)Kd10.000011
su 11248Homo sapiens (human)Kd10.000022
vx680Homo sapiens (human)Kd10.000011
axitinibHomo sapiens (human)Kd10.000011
pd 184352Homo sapiens (human)Kd10.000011
bms345541Homo sapiens (human)Kd0.130011
midostaurinHomo sapiens (human)Kd8.150022
ki 20227Homo sapiens (human)Kd10.000011
pi103Homo sapiens (human)Kd10.000011
hki 272Homo sapiens (human)Kd10.000011
tofacitinibHomo sapiens (human)Kd10.000011
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd0.019011
cediranibHomo sapiens (human)Kd10.000011
masitinibHomo sapiens (human)Kd10.000011
pazopanibHomo sapiens (human)Kd10.000011
azd 6244Homo sapiens (human)Kd10.000011
su 14813Homo sapiens (human)Kd5.300011
bibw 2992Homo sapiens (human)Kd10.000011
tg100-115Homo sapiens (human)Kd10.000011
pha 665752Homo sapiens (human)Kd10.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd0.071011
brivanibHomo sapiens (human)Kd10.000011
at 7519Homo sapiens (human)Kd10.000011
bi 2536Homo sapiens (human)Kd10.000011
nvp-ast487Homo sapiens (human)Kd0.110011
kw 2449Homo sapiens (human)Kd0.430011
abt 869Homo sapiens (human)Kd10.000011
gw 2580Homo sapiens (human)Kd10.000011
crizotinibHomo sapiens (human)Kd5.500011
chir-265Homo sapiens (human)Kd10.000011
motesanibHomo sapiens (human)Kd10.000011
mln8054Homo sapiens (human)Kd10.000011
GDC-0879Homo sapiens (human)Kd10.000011
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd10.000011
nvp-tae684Homo sapiens (human)Kd10.000011
fedratinibHomo sapiens (human)Kd0.360011
gsk690693Homo sapiens (human)Kd10.000011
gdc 0941Homo sapiens (human)Kd10.000011
plx 4720Homo sapiens (human)Kd10.000011
sgx 523Homo sapiens (human)Kd10.000011
quizartinibHomo sapiens (human)Kd10.000022
incb-018424Homo sapiens (human)Kd2.300011
gsk 1838705aHomo sapiens (human)Kd10.000011
gsk 1363089Homo sapiens (human)Kd10.000011
chir 258Homo sapiens (human)Kd10.000011
nintedanibHomo sapiens (human)Kd10.000011
pp242Homo sapiens (human)Kd10.000011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
salicylic acidHomo sapiens (human)INH1,000.000011

Enables

This protein enables 12 target(s):

TargetCategoryDefinition
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
protein serine/threonine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
IkappaB kinase activitymolecular functionCatalysis of the reaction: ATP + IkappaB protein = ADP + IkappaB phosphoprotein. [EC:2.7.11.10]
protein kinase bindingmolecular functionBinding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [GOC:jl]
protein heterodimerization activitymolecular functionBinding to a nonidentical protein to form a heterodimer. [GOC:ai]
scaffold protein bindingmolecular functionBinding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
transferrin receptor bindingmolecular functionBinding to a transferrin receptor. [GOC:pm, PMID:9819414]

Located In

This protein is located in 4 target(s):

TargetCategoryDefinition
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
cytoplasmic side of plasma membranecellular componentThe leaflet the plasma membrane that faces the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb]
membrane raftcellular componentAny of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Part Of

This protein is part of 2 target(s):

TargetCategoryDefinition
IkappaB kinase complexcellular componentA trimeric protein complex that phosphorylates inhibitory-kappaB (I-kappaB) proteins. The complex is composed of two kinase subunits (alpha and beta) and a regulatory gamma subunit (also called NEMO). In a resting state, NF-kappaB dimers are bound to inhibitory IKB proteins, sequestering NF-kappaB in the cytoplasm. Phosphorylation of I-kappaB targets I-kappaB for ubiquitination and proteasomal degradation, thus releasing the NF-kappaB dimers, which can translocate to the nucleus to bind DNA and regulate transcription. [GOC:bf, GOC:ma, PMID:12055104, PMID:20300203]
CD40 receptor complexcellular componentA protein complex that contains at least CD40 (a cell surface receptor of the tumour necrosis factor receptor (TNFR) superfamily), and other signaling molecules. [GOC:BHF, PMID:20614026, PMID:9221764]

Involved In

This protein is involved in 29 target(s):

TargetCategoryDefinition
stimulatory C-type lectin receptor signaling pathwaybiological processThe series of molecular signals initiated by the binding of C-type lectin to its receptor on the surface of a target cell, and resulting in cellular activation. [GO_REF:0000022, GOC:add, ISBN:0781735149]
antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependentbiological processThe process in which an antigen-presenting cell expresses a peptide antigen of exogenous origin on its cell surface in association with an MHC class I protein complex following intracellular transport via a TAP (transporter associated with antigen processing) pathway. The peptide is typically a fragment of a larger exogenous protein which has been degraded within the cell and is dependent on TAP transport from the cytosol to ER for association with the MHC class I molecule. Class I here refers to classical class I molecules. [GOC:add, PMID:15224093, PMID:15771591, PMID:16181335]
MyD88-dependent toll-like receptor signaling pathwaybiological processA toll-like receptor signaling pathway in which the MyD88 adaptor molecule mediates transduction of the signal. Toll-like receptors directly bind pattern motifs from a variety of microbial sources to initiate an innate immune response. [GOC:add, ISBN:0781735149, PMID:12467241, PMID:12524386, PMID:12855817, PMID:15585605, PMID:15728447]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
inflammatory responsebiological processThe immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732]
canonical NF-kappaB signal transductionbiological processAn intracellular signaling cassette characterized by the I-kappaB-kinase (IKK)-dependent activation of NF-kappaB, also known as the canonical NF-kappaB signaling cascade. The cascade begins with activation of a trimeric IKK complex (consisting of catalytic kinase subunits IKKalpha and/or IKKbeta, and the regulatory scaffold protein NEMO) and ends with the regulation of transcription of target genes by NF-kappaB. In a resting state, NF-kappaB dimers are bound to I-kappaB proteins, sequestering NF-kappaB in the cytoplasm. Phosphorylation of I-kappaB targets I-kappaB for ubiquitination and proteasomal degradation, thus releasing the NF-kappaB dimers, which can translocate to the nucleus to bind DNA and regulate transcription. The canonical NF-kappaB pathway is mainly stimulated by proinflammatory cytokines such as IL-1beta, tumor necrosis factor (TNF)-alpha, antigen ligands, and toll-like receptors (TLRs). [GOC:bf, PMID:12773372, PMID:34659217]
response to virusbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a virus. [GOC:hb]
regulation of tumor necrosis factor-mediated signaling pathwaybiological processAny process that modulates the rate or extent of the tumor necrosis factor-mediated signaling pathway. The tumor necrosis factor-mediated signaling pathway is the series of molecular signals generated as a consequence of tumor necrosis factor binding to a cell surface receptor. [GOC:dph, GOC:tb]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
cortical actin cytoskeleton organizationbiological processA process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of actin-based cytoskeletal structures in the cell cortex, i.e. just beneath the plasma membrane. [GOC:dph, GOC:jl, GOC:mah, GOC:pf]
tumor necrosis factor-mediated signaling pathwaybiological processThe series of molecular signals initiated by tumor necrosis factor binding to its receptor on the surface of a cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling]
toll-like receptor 3 signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to the endolysosomal toll-like receptor 3. [GOC:add, PMID:16551253, PMID:17328678]
negative regulation of myosin-light-chain-phosphatase activitybiological processAny process that stops, prevents, or reduces the frequency, rate or extent of myosin-light-chain-phosphatase activity. [GOC:bf, GOC:go_curators]
TRIF-dependent toll-like receptor signaling pathwaybiological processThe series of molecular signals initiated by a ligand binding to a toll-like receptor where the TRIF adaptor mediates transduction of the signal. Toll-like receptors directly bind pattern motifs from a variety of microbial sources to initiate an innate immune response. [GOC:BHF, PMID:12855817]
Fc-epsilon receptor signaling pathwaybiological processThe series of molecular signals initiated by the binding of the Fc portion of immunoglobulin E (IgE) to an Fc-epsilon receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. The Fc portion of an immunoglobulin is its C-terminal constant region. [GOC:phg, PMID:12413516, PMID:15048725]
regulation of phosphorylationbiological processAny process that modulates the frequency, rate or extent of addition of phosphate groups into a molecule. [GOC:jl]
positive regulation of canonical NF-kappaB signal transductionbiological processAny process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
innate immune responsebiological processInnate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu]
positive regulation of DNA-templated transcriptionbiological processAny process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
T cell receptor signaling pathwaybiological processThe series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add]
positive regulation of NF-kappaB transcription factor activitybiological processAny process that activates or increases the frequency, rate or extent of activity of the transcription factor NF-kappaB. [GOC:dph, GOC:tb, PMID:15087454, PMID:15170030]
stress-activated MAPK cascadebiological processA MAPK cascade that starts with the activation of a stress-activated MAP kinase cascade. [GOC:ai, PMID:15936270]
protein maturationbiological processAny process leading to the attainment of the full functional capacity of a protein. [GOC:ai]
interleukin-1-mediated signaling pathwaybiological processThe series of molecular signals initiated by interleukin-1 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling]
cellular response to tumor necrosis factorbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a tumor necrosis factor stimulus. [GOC:mah]
protein localization to plasma membranebiological processA process in which a protein is transported to, or maintained in, a specific location in the plasma membrane. [GOC:mah]
regulation of establishment of endothelial barrierbiological processAny process that modulates the frequency, rate or extent of establishment of endothelial barrier. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:24851274]
negative regulation of bicellular tight junction assemblybiological processAny process that stops, prevents or reduces the frequency, rate or extent of tight junction assembly. [GO_REF:0000058, GOC:jz, GOC:TermGenie, PMID:25050009]