Proteins > Dual specificity mitogen-activated protein kinase kinase 4
Page last updated: 2024-08-07 13:18:05

Dual specificity mitogen-activated protein kinase kinase 4

A dual specificity mitogen-activated protein kinase kinase 4 that is encoded in the genome of human. [TLR:AMM, UniProtKB:P45985]

Synonyms

MAP kinase kinase 4;
MAPKK 4;
EC 2.7.12.2;
JNK-activating kinase 1;
MAPK/ERK kinase 4;
MEK 4;
SAPK/ERK kinase 1;
SEK1;
Stress-activated protein kinase kinase 1;
SAPK kinase 1;
SAPKK-1;
SAPKK1;
c-Jun N-termi

Research

Bioassay Publications (10)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (40.00)29.6817
2010's5 (50.00)24.3611
2020's1 (10.00)2.80

Compounds (144)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.863033
genisteinHomo sapiens (human)IC500.400011
sl 327Homo sapiens (human)IC5010.000011
fr 148083Homo sapiens (human)IC503.000011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
sb 202190Homo sapiens (human)Kd10.000011
imatinibHomo sapiens (human)Kd16.666733
staurosporineHomo sapiens (human)Kd0.070022
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.265933
vatalanibHomo sapiens (human)Kd16.666733
ruboxistaurinHomo sapiens (human)Kd0.930022
canertinibHomo sapiens (human)Kd10.000022
birb 796Homo sapiens (human)Kd10.000022
cyc 202Homo sapiens (human)Kd20.000022
sb 203580Homo sapiens (human)Kd10.000022
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd16.666733
lapatinibHomo sapiens (human)Kd10.000022
sorafenibHomo sapiens (human)Kd10.000033
pd 173955Homo sapiens (human)Kd0.330011
s 1033Homo sapiens (human)Kd10.000011
bms 387032Homo sapiens (human)Kd10.000022
sf 2370Homo sapiens (human)Kd30.000011
tandutinibHomo sapiens (human)Kd10.000033
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd10.000022
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000012
zd 6474Homo sapiens (human)Kd10.000022
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd14.100033
bosutinibHomo sapiens (human)Kd16.300022
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd6.900033
palbociclibHomo sapiens (human)Kd1.251011
jnj-7706621Homo sapiens (human)Kd0.630011
vx680Homo sapiens (human)Kd16.666733
cyc 116Homo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd20.000022
axitinibHomo sapiens (human)Kd10.000011
temsirolimusHomo sapiens (human)Kd30.000011
pd 184352Homo sapiens (human)Kd10.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000011
bms345541Homo sapiens (human)Kd10.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd4.800033
ki 20227Homo sapiens (human)Kd10.000011
cp 724714Homo sapiens (human)Kd10.000011
pi103Homo sapiens (human)Kd10.000022
tivozanibHomo sapiens (human)Kd30.000012
hki 272Homo sapiens (human)Kd10.000011
tofacitinibHomo sapiens (human)Kd10.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd20.000022
masitinibHomo sapiens (human)Kd20.000022
pazopanibHomo sapiens (human)Kd10.393333
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd1.400022
bibw 2992Homo sapiens (human)Kd10.000011
binimetinibHomo sapiens (human)Kd30.000011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000012
crenolanibHomo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd4.000011
exel-7647Homo sapiens (human)Kd30.000011
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)Kd15.100022
brivanibHomo sapiens (human)Kd10.000011
mp470Homo sapiens (human)Kd30.000012
at 7519Homo sapiens (human)Kd10.000011
bms-690514Homo sapiens (human)Kd30.000011
bi 2536Homo sapiens (human)Kd20.000022
inno-406Homo sapiens (human)Kd30.000011
nvp-ast487Homo sapiens (human)Kd5.500022
kw 2449Homo sapiens (human)Kd15.125022
danusertibHomo sapiens (human)Kd30.000011
abt 869Homo sapiens (human)Kd16.666733
azd 8931Homo sapiens (human)Kd30.000011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
gw 2580Homo sapiens (human)Kd10.000022
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd23.333323
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd16.666733
motesanibHomo sapiens (human)Kd10.000022
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd16.666733
GDC-0879Homo sapiens (human)Kd10.000011
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd16.666733
nvp-tae684Homo sapiens (human)Kd0.150011
enmd 2076Homo sapiens (human)Kd30.000011
tak-901Homo sapiens (human)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd30.000011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd9.900011
gsk690693Homo sapiens (human)Kd10.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd20.000022
icotinibHomo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000011
plx 4720Homo sapiens (human)Kd0.190011
mk 5108Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd30.000011
sgx 523Homo sapiens (human)Kd10.000011
amg 900Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd10.000022
tak 733Homo sapiens (human)Kd30.000011
sns 314Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd1.800011
TAK-580Homo sapiens (human)Kd0.146011
emd1214063Homo sapiens (human)Kd30.000011
gsk 1838705aHomo sapiens (human)Kd0.910011
pf 3758309Homo sapiens (human)Kd30.000011
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolHomo sapiens (human)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd20.000022
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000011
dabrafenibHomo sapiens (human)Kd30.000011
n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamideHomo sapiens (human)Kd30.000011
ribociclibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000012
glpg0634Homo sapiens (human)Kd30.000011
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd30.000011
chir 258Homo sapiens (human)Kd16.666733
nintedanibHomo sapiens (human)Kd16.850022
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd0.810011

Enables

This protein enables 8 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 tyrosine kinase activitymolecular functionCatalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596]
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]
JUN kinase kinase activitymolecular functionCatalysis of the phosphorylation of tyrosine and threonine residues in a c-Jun NH2-terminal kinase (JNK), a member of a subgroup of mitogen-activated protein kinases (MAPKs), which signal in response to cytokines and exposure to environmental stress. JUN kinase kinase (JNKK) is a dual-specificity protein kinase kinase and requires activation by a serine/threonine kinase JUN kinase kinase kinase. [GOC:bf, PMID:11057897, PMID:11790549]
molecular adaptor activitymolecular functionThe binding activity of a molecule that brings together two or more molecules through a selective, non-covalent, often stoichiometric interaction, permitting those molecules to function in a coordinated way. [GOC:mtg_MIT_16mar07, GOC:vw]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 5 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]
axoncellular componentThe long process of a neuron that conducts nerve impulses, usually away from the cell body to the terminals and varicosities, which are sites of storage and release of neurotransmitter. [GOC:nln, ISBN:0198506732]
dendrite cytoplasmcellular componentAll of the contents of a dendrite, excluding the surrounding plasma membrane. [GOC:mah]
perikaryoncellular componentThe portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl]

Involved In

This protein is involved in 17 target(s):

TargetCategoryDefinition
positive regulation of protein phosphorylationbiological processAny process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd]
signal transductionbiological processThe cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11]
JNK cascadebiological processA MAPK cascade containing at least the JNK (MAPK8) MAP kinase. It starts with the activation of JUN3K (a MAPK3K), which activates JNKK a MAP2K), which in turn activates JNK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinases in the downstream tier. The JNK cascade is activated by stress signals, as well as by G protein-coupled receptors, growth factors, and cytokines, and results in cellular responses such as cell proliferation, cell differentiation, apoptosis and inflammation. [PMID:11790549, PMID:20811974, PMID:23125017]
response to woundingbiological 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 indicating damage to the organism. [GOC:go_curators]
smooth muscle cell apoptotic processbiological processAny apoptotic process in a smooth muscle cell. Smooth muscle consists of non-striated, elongated, spindle-shaped cell found lining the digestive tract, uterus, and blood vessels. [CL:0000192, GOC:BHF, GOC:mah, GOC:mtg_apoptosis, GOC:rl]
intrinsic apoptotic signaling pathway in response to hydrogen peroxidebiological processThe series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced in response to hydrogen peroxide (H2O2). [GOC:bf, GOC:PARL]
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]
positive regulation of neuron apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis]
positive regulation of DNA replicationbiological processAny process that activates or increases the frequency, rate or extent of DNA replication. [GOC:go_curators]
positive regulation of JNK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the JNK cascade. [GOC:bf]
positive regulation of nitric-oxide synthase biosynthetic processbiological processAny process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of a nitric oxide synthase enzyme. [GOC:ai]
cell growth involved in cardiac muscle cell developmentbiological processThe growth of a cardiac muscle cell, where growth contributes to the progression of the cell over time from its initial formation to its mature state. [GOC:dph]
cellular response to mechanical stimulusbiological 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 mechanical stimulus. [GOC:mah]
cellular response to sorbitolbiological 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 sorbitol stimulus. [GOC:mah]
cellular senescencebiological processA cell aging process stimulated in response to cellular stress, whereby normal cells lose the ability to divide through irreversible cell cycle arrest. [GOC:BHF, PMID:28682291]
negative regulation of motor neuron apoptotic processbiological processAny process that stops, prevents or reduces the frequency, rate or extent of motor neuron apoptotic process. [GOC:mtg_apoptosis, GOC:obol]
MAPK cascadebiological processAn intracellular protein kinase cascade containing at least a MAP kinase (MAPK). It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and a MAPK. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier to transmit a signal within a cell. [PMID:20811974, PMID:9561267]