Page last updated: 2024-08-07 10:25:35

Serine/threonine-protein kinase/endoribonuclease IRE2

A serine/threonine-protein kinase/endoribonuclease IRE2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q76MJ5]

Synonyms

Endoplasmic reticulum-to-nucleus signaling 2;
Inositol-requiring protein 2;
hIRE2p;
Ire1-beta;
IRE1b

Research

Bioassay Publications (3)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (100.00)24.3611
2020's0 (0.00)2.80

Compounds (211)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
staurosporineHomo sapiens (human)IC500.041622

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
fasudilHomo sapiens (human)Kd30.000011
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
imatinibHomo sapiens (human)Kd30.000011
triciribine phosphateHomo sapiens (human)Kd30.000011
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd30.000011
lestaurtinibHomo sapiens (human)Kd0.292011
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd30.000011
ruboxistaurinHomo sapiens (human)Kd30.000011
canertinibHomo sapiens (human)Kd30.000011
cyc 202Homo sapiens (human)Kd30.000011
enzastaurinHomo sapiens (human)Kd30.000011
erlotinibHomo sapiens (human)Kd30.000011
lapatinibHomo sapiens (human)Kd30.000011
s 1033Homo sapiens (human)Kd30.000011
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd30.000011
sf 2370Homo sapiens (human)Kd0.908011
tandutinibHomo sapiens (human)Kd30.000011
dasatinibHomo sapiens (human)Kd30.000011
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd30.000011
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd30.000011
bosutinibHomo sapiens (human)Kd30.000011
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd30.000011
palbociclibHomo sapiens (human)Kd30.000011
vx680Homo sapiens (human)Kd30.000011
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd30.000011
axitinibHomo sapiens (human)Kd30.000011
temsirolimusHomo sapiens (human)Kd30.000011
on 01910Homo sapiens (human)Kd30.000011
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000012
midostaurinHomo sapiens (human)Kd30.000011
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000011
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd30.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000012
hki 272Homo sapiens (human)Kd30.000011
tofacitinibHomo sapiens (human)Kd30.000011
cediranibHomo sapiens (human)Kd30.000011
masitinibHomo sapiens (human)Kd30.000011
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd30.000011
azd 6244Homo sapiens (human)Kd30.000011
su 14813Homo sapiens (human)Kd30.000011
bibw 2992Homo sapiens (human)Kd30.000011
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd30.000012
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd30.000011
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
azd 7762Homo sapiens (human)Kd30.000011
regorafenibHomo sapiens (human)Kd30.000011
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)Kd30.000011
brivanibHomo sapiens (human)Kd30.000011
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd30.000011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd30.000012
bms-690514Homo sapiens (human)Kd30.000012
bi 2536Homo sapiens (human)Kd30.000011
inno-406Homo sapiens (human)Kd30.000011
kw 2449Homo sapiens (human)Kd30.000011
danusertibHomo sapiens (human)Kd30.000011
abt 869Homo sapiens (human)Kd30.000011
azd 8931Homo sapiens (human)Kd30.000011
arq 197Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd30.000011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.000011
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamideHomo sapiens (human)Kd30.000011
cc-930Homo sapiens (human)Kd30.000012
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd30.000011
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd30.000011
motesanibHomo sapiens (human)Kd30.000012
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd30.000011
pf-562,271Homo sapiens (human)Kd30.000011
jnj-26483327Homo sapiens (human)Kd30.000011
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000011
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd30.000011
azd 1152-hqpaHomo sapiens (human)Kd30.000011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd0.986011
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinoneHomo sapiens (human)Kd30.000011
tak-901Homo sapiens (human)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo 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)Kd30.000012
gsk690693Homo sapiens (human)Kd30.000011
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaeneHomo sapiens (human)Kd30.000011
azd5438Homo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd30.000011
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000012
mk 5108Homo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd30.000011
cudc 101Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd30.000011
tak 593Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd30.000011
sgx 523Homo sapiens (human)Kd30.000011
bms 777607Homo sapiens (human)Kd30.000011
sgi 1776Homo sapiens (human)Kd30.000011
pci 32765Homo sapiens (human)Kd30.000011
ponatinibHomo sapiens (human)Kd30.000011
amg 900Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd30.000011
tak 733Homo sapiens (human)Kd30.000011
mk 2206Homo sapiens (human)Kd30.000011
sns 314Homo sapiens (human)Kd30.000011
lucitanibHomo sapiens (human)Kd30.000011
pf-04691502Homo sapiens (human)Kd30.000011
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamideHomo sapiens (human)Kd30.000011
dcc-2036Homo sapiens (human)Kd30.000011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd30.000011
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd30.000011
entrectinibHomo sapiens (human)Kd30.000011
pexidartinibHomo sapiens (human)Kd30.000011
TAK-580Homo sapiens (human)Kd30.000011
gsk 2126458Homo sapiens (human)Kd30.000011
emd1214063Homo sapiens (human)Kd30.000011
pf 3758309Homo sapiens (human)Kd30.000011
gdc 0980Homo sapiens (human)Kd30.000011
azd2014Homo 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)Kd30.000011
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
mk 2461Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000012
baricitinibHomo sapiens (human)Kd30.000011
dabrafenibHomo sapiens (human)Kd0.116011
pki 587Homo 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
mk-8033Homo sapiens (human)Kd30.000011
pha 793887Homo sapiens (human)Kd30.000012
sb 1518Homo sapiens (human)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000012
gsk 1070916Homo sapiens (human)Kd30.000012
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd30.000011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000011
gsk2141795Homo sapiens (human)Kd30.000011
azd8186Homo sapiens (human)Kd1.500011
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd30.000011
azd1208Homo sapiens (human)Kd30.000011
vx-509Homo sapiens (human)Kd30.000011
debio 1347Homo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd30.000011
otssp167Homo sapiens (human)Kd30.000011
chir 258Homo sapiens (human)Kd30.000011
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd30.000011
bay 80-6946Homo sapiens (human)Kd30.000011

Enables

This protein enables 7 target(s):

TargetCategoryDefinition
magnesium ion bindingmolecular functionBinding to a magnesium (Mg) ion. [GOC:ai]
endonuclease activitymolecular functionCatalysis of the hydrolysis of ester linkages within nucleic acids by creating internal breaks. [GOC:mah, ISBN:0198547684]
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]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]
RNA endonuclease activitymolecular functionCatalysis of the hydrolysis of ester linkages within ribonucleic acid by creating internal breaks. [GOC:mah, ISBN:0198547684]
unfolded protein bindingmolecular functionBinding to an unfolded protein. [GOC:ai]

Located In

This protein is located in 3 target(s):

TargetCategoryDefinition
endoplasmic reticulumcellular componentThe irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732]
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]
endoplasmic reticulum quality control compartmentcellular componentA subcompartment of the endoplasmic reticulum in which proteins with improper or incorrect folding accumulate. Enzymes in this compartment direct proteins with major folding problems to translocation to the cytosol and degradation, and proteins with minor folding problems to the ER, to interact with chaperon proteins. [PMID:11408579]

Part Of

This protein is part of 1 target(s):

TargetCategoryDefinition
IRE1-TRAF2-ASK1 complexcellular componentA protein complex of the endoplasmic reticulum membrane that consists of IRE1 (Inositol-requiring enzyme-1), TRAF2 (TNF receptor-associated factor 2) and ASK1 (Apoptosis signal-regulating kinase 1, a MAP3K). [GOC:bf, GOC:PARL, PMID:12050113, PMID:23000344]

Involved In

This protein is involved in 8 target(s):

TargetCategoryDefinition
mRNA processingbiological processAny process involved in the conversion of a primary mRNA transcript into one or more mature mRNA(s) prior to translation into polypeptide. [GOC:mah]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
rRNA catabolic processbiological processThe chemical reactions and pathways resulting in the breakdown of rRNA, ribosomal RNA, a structural constituent of ribosomes. [GOC:ai]
apoptotic chromosome condensationbiological processThe compaction of chromatin during apoptosis. [GOC:mah]
response to endoplasmic reticulum stressbiological 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 stress acting at the endoplasmic reticulum. ER stress usually results from the accumulation of unfolded or misfolded proteins in the ER lumen. [GOC:cjm, GOC:mah]
negative regulation of DNA-templated transcriptionbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH]
IRE1-mediated unfolded protein responsebiological processThe series of molecular signals mediated by the endoplasmic reticulum stress sensor IRE1 (Inositol-requiring transmembrane kinase/endonuclease). Begins with activation of IRE1 in response to endoplasmic reticulum (ER) stress, and ends with regulation of a downstream cellular process, e.g. transcription. One target of activated IRE1 is the transcription factor HAC1 in yeast, or XBP1 in mammals; IRE1 cleaves an intron of a mRNA coding for HAC1/XBP1 to generate an activated HAC1/XBP1 transcription factor, which controls the up regulation of UPR-related genes. At least in mammals, IRE1 can also signal through additional intracellular pathways including JNK and NF-kappaB. [GOC:bf, GOC:PARL, PMID:22013210]
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressbiological 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 a stimulus indicating endoplasmic reticulum (ER) stress, and ends when the execution phase of apoptosis is triggered. ER stress usually results from the accumulation of unfolded or misfolded proteins in the ER lumen. [GOC:mah, GOC:mtg_apoptosis, PMID:18701708]