Information on EC 2.7.12.2 - mitogen-activated protein kinase kinase

for references in articles please use BRENDA:EC2.7.12.2
Word Map on EC 2.7.12.2
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:

The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.12.2
-
RECOMMENDED NAME
GeneOntology No.
mitogen-activated protein kinase kinase
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (MAPKKK-activated)
This enzyme is a dual-specific protein kinase and requires mitogen-activated protein kinase kinase kinase (MAPKKK) for activation. It is required for activation of EC 2.7.11.24, mitogen-activated protein kinase. Phosphorylation of MEK1 by Raf involves phosphorylation of two serine residues [5]. Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumour necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischaemic injury.
CAS REGISTRY NUMBER
COMMENTARY hide
142805-58-1
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
i.e. Botryotinia fuckeliana
UniProt
Manually annotated by BRENDA team
i.e. Botryotinia fuckeliana
UniProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
cv. Tainung 57
-
-
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
cvs. SF43 and Nipponbare
UniProt
Manually annotated by BRENDA team
MKK6a; the fish does not possess a MKK3 gene
UniProt
Manually annotated by BRENDA team
-
UniProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
isolated from a smoke tree, Cotinuscoggygria in Fragrant Hills Park,Beijing
-
-
Manually annotated by BRENDA team
isolated from a smoke tree, Cotinuscoggygria in Fragrant Hills Park,Beijing
-
-
Manually annotated by BRENDA team
cv. Zhengdan 958
UniProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + BcSak1
ADP + phosphorylated BcSak1
show the reaction diagram
ATP + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
show the reaction diagram
ATP + casein
ADP + phosphorylated casein
show the reaction diagram
-
-
-
?
ATP + ERK
ADP + phospho-ERK
show the reaction diagram
-
-
-
-
?
ATP + ERK
ADP + phosphorylated ERK
show the reaction diagram
ATP + Erk-1 gene product
ADP + phosphorylated Erk-1 gene product
show the reaction diagram
phosphorylation primarily on a tyrosine residue and, to a lesser extent, on a threonine
-
?
ATP + ERK1
ADP + phosphorylated ERK1
show the reaction diagram
ATP + ERK1/2
ADP + phosphorylated ERK1/2
show the reaction diagram
-
-
-
-
?
ATP + ERK2
ADP + phosphorylated ERK2
show the reaction diagram
ATP + extracellular regulated kinase 1
ADP + phosphorylated extracellular regulated kinase 1
show the reaction diagram
-
-
-
?
ATP + extracellular regulated kinase 2
ADP + phosphorylated extracellular regulated kinase 2
show the reaction diagram
-
-
-
?
ATP + GhMPK7
ADP + phosphorylated GhMPK7
show the reaction diagram
-
-
-
?
ATP + Janus kinase 2
ADP + phospho-Janus kinase 2
show the reaction diagram
-
activation
-
-
?
ATP + JNK
ADP + JNK phosphate
show the reaction diagram
ATP + JNK
ADP + phopsho-JNK
show the reaction diagram
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
show the reaction diagram
ATP + JNK
ADP + phosphorylated JNK
show the reaction diagram
ATP + JNK1
ADP + phosphorylated JNK1
show the reaction diagram
ATP + K52R-[ERK2]
ADP + phospho-K52R-[ERK2]
show the reaction diagram
-
catalytically inactive ERK2 in which lysine-52 is substituted with arginine
-
-
?
ATP + K53M-[p38alpha]
ADP + phospho-K53M-[p38alpha]
show the reaction diagram
-
catalytically inactive p38alpha in which lysine-53 is substituted with methionine
-
-
?
ATP + KIMPK3
ADP + phosphorylated KIMPK3
show the reaction diagram
-
-
-
-
?
ATP + KIMPK6
ADP + phosphorylated KIMPK6
show the reaction diagram
-
-
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
show the reaction diagram
ATP + MAP kinase 6
ADP + phosphorylated Map kinase 6
show the reaction diagram
Arabidopsis thaliana MAP kinase MPK6
-
-
?
ATP + MAP kinase ERK1
ADP + ?
show the reaction diagram
-
-
-
?
ATP + MAPK
ADP + phosphorylated MAPK
show the reaction diagram
ATP + MKK4
ADP + phosphorylated MKK4
show the reaction diagram
-
-
-
-
?
ATP + MPK-7
ADP + phospho-MPK-7
show the reaction diagram
ATP + myelin basic protein
ADP + phoshorylated myelin basic protein
show the reaction diagram
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
ATP + myelin basic protein kinase
ADP + phosphorylated myelin basic protein kinase
show the reaction diagram
-
-
-
?
ATP + MyoD
ADP + phospharylated MyoD
show the reaction diagram
ATP + p38
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + p38
ADP + p38 phosphate
show the reaction diagram
ATP + p38
ADP + phospho-p38
show the reaction diagram
ATP + p38
ADP + phosphorylated p38
show the reaction diagram
-
-
-
-
?
ATP + p38 MAP kinase
ADP + ?
show the reaction diagram
-
phosphorylates and activates p38 MAP kinase
-
-
?
ATP + p38/MPK2 kinase
ADP + ?
show the reaction diagram
-
phosphorylates and specifically activates the p38/MPK2 subgroup of the mitogen-activated protein kinase superfamily
-
-
?
ATP + p38alpha
ADP + phosphorylated p38alpha
show the reaction diagram
-
MKK6 phosphorylates p38 MAPK on Thr180 and Tyr182, the sites of phosphorylation that activate p38 MAPK
-
-
?
ATP + p42 MAP kinase
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + Pfmap2
ADP + phosphorylated Pfmap2
show the reaction diagram
-
the enzyme phosphorylates its potential in vivo Pfmap2 substrate largely on Thr290
-
-
?
ATP + poly-(Tyr-Glu)
ADP + phospho-poly-(Tyr-Glu)
show the reaction diagram
-
tyrosine kinase substrate
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + Red1
ADP + phospho-Red1
show the reaction diagram
-
substrate of Mek1
-
-
?
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
ATP + VdHog1
ADP + phosphorylated VdHog1
show the reaction diagram
ATP + [ERK2 substrate peptide]
ADP + [ERK2 substrate peptide] phosphate
show the reaction diagram
-
MEK1
-
-
?
ATP + [myelin basic protein substrate peptide]
ADP + [myelin basic protein substrate peptide] phosphate
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + BcSak1
ADP + phosphorylated BcSak1
show the reaction diagram
ATP + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
show the reaction diagram
ATP + ERK
ADP + phospho-ERK
show the reaction diagram
-
-
-
-
?
ATP + ERK
ADP + phosphorylated ERK
show the reaction diagram
ATP + ERK1
ADP + phosphorylated ERK1
show the reaction diagram
-
phosphorylation of extracellular signal-regulated kinase 1
-
-
?
ATP + ERK1/2
ADP + phosphorylated ERK1/2
show the reaction diagram
-
-
-
-
?
ATP + ERK2
ADP + phosphorylated ERK2
show the reaction diagram
ATP + extracellular regulated kinase 1
ADP + phosphorylated extracellular regulated kinase 1
show the reaction diagram
I3L5D4
-
-
-
?
ATP + extracellular regulated kinase 2
ADP + phosphorylated extracellular regulated kinase 2
show the reaction diagram
I3L5D4
-
-
-
?
ATP + GhMPK7
ADP + phosphorylated GhMPK7
show the reaction diagram
S4S5K3
-
-
-
?
ATP + Janus kinase 2
ADP + phospho-Janus kinase 2
show the reaction diagram
-
activation
-
-
?
ATP + JNK
ADP + JNK phosphate
show the reaction diagram
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + JNK
ADP + phopsho-JNK
show the reaction diagram
P47809, Q8CE90
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
show the reaction diagram
ATP + JNK
ADP + phosphorylated JNK
show the reaction diagram
ATP + MAP kinase
ADP + phosphorylated MAP kinase
show the reaction diagram
ATP + MAPK
ADP + phosphorylated MAPK
show the reaction diagram
ATP + MPK-7
ADP + phospho-MPK-7
show the reaction diagram
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
Pfnek3 phosphorylates MBP on threonine, but not serine residues
-
-
?
ATP + MyoD
ADP + phospharylated MyoD
show the reaction diagram
-
phosphorylation at Tyr156, activated MEK1 associates with MyoD
-
-
?
ATP + p38
ADP + p38 phosphate
show the reaction diagram
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + p38
ADP + phospho-p38
show the reaction diagram
ATP + p38alpha
ADP + phosphorylated p38alpha
show the reaction diagram
-
MKK6 phosphorylates p38 MAPK on Thr180 and Tyr182, the sites of phosphorylation that activate p38 MAPK
-
-
?
ATP + Pfmap2
ADP + phosphorylated Pfmap2
show the reaction diagram
-
the enzyme phosphorylates its potential in vivo Pfmap2 substrate largely on Thr290
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
-
mitogen-activated protein kinase kinase-1 regulates SMAD3 expression in epithelial and smooth muscle cells, which is stimulated by TGFbeta-1, SMAD3 is a transcription factor that mediates TGF-?1 signaling and is important in many of the cellular processes that regulate fibrosis and inflammation, overview
-
-
?
ATP + VdHog1
ADP + phosphorylated VdHog1
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
elevation of cytosolic Ca2+ by ethylene may stimulate protein phosphatase and MAPKK, which finally activates IPO expression
Cd2+
-
can partially substitue Mg2+
Co2+
-
can partially substitue Mg2+
NaCl
mitogen-activated protein kinase kinase 5, MKK5, is activated in response to salt stress
additional information
-
serine/threonine and tyrosine kinase activities are distinctly influenced by Mg2+ and Mn2+ cofactors. Pfnek3 can undergo further tyrosine autophosphorylation in vitro, with Mn2+ as the preferred metal cofactor
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(2,3-dihydroxypropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
-
1-(3-cyanopropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
1-allyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
1-ethyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
1-methyl-4-(2-naphthylamino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
-
3,4-difluoro-N-(3-{5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3-phenyl-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)-5-hydroxybenzamide
-
-
3,4-difluoro-N-{3-[3-(3-fluoro-4-hydroxyphenyl)-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-5-hydroxybenzamide
-
-
3,4-difluoro-N-{3-[5-({2-fluoro-4-[(hydroxymethyl)amino]phenyl}amino)-3-(3-fluoro-4-hydroxyphenyl)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-5-hydroxybenzamide
-
-
3,4-difluoro-N-{3-[5-{[2-fluoro-4-(formylamino)phenyl]amino}-3-(3-fluoro-4-hydroxyphenyl)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-5-hydroxybenzamide
-
-
4-(2-fluoro-4-iodoanilino)-1-(2-hydroxyethyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-1-(3-hydroxypropyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylic acid
;
4-(2-fluoro-4-iodoanilino)-1-[2-(2-methoxyethoxy)ethyl]-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-6-oxo-1-propyl-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-N,1-dimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-N,N,1-trimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
-
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-iodoanilino)-N-(3-hydroxypropyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-methylanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(2-fluoro-4-methylsulfanylphenylamino)-1-methyl-6-oxo-1,6-dihydro-3 -pyridinecarboxamide
;
4-(3,4-dichlorophenylamino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(4-bromo-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(4-bromo-2-fluoroanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-one
-
selective anthranilic acid type inhibitors, residues K97, I141, M143, F129, V127, I126, L118, F209, V211, and S212 of MEK1/2 are important for interaction with the inhibitor, noncompetitive to ATP, inhibition of ERK phosphorylation by MEK1/2 by the derivatives with IC50 values of 6.8-124 nM, low cytotoxic effects, overview
4-(4-cyano-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(4-ethyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-(4-ethynyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-amino-1-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl]-2-hydroxybutan-1-one
-
4-[2-fluoro-4-(1,1,2,2,3,3,4,4,4-nonafluorobutyl)anilino]-1-methyl-6-oxo-1,6 -dihydro-3-pyridinecarboxamide
;
4-[2-fluoro-4-(3-hydroxypropyl)anilino]-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
;
4-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl]-3-hydroxy-4-oxobutanamide
-
anthrax lethal toxin
-
i.e. LeTx, inactivates MKKs, LeTx treatment reduces the levels of phosphorylated extracellular signal-regulated kinase and p38 MAPK in vitro, short treatments with LeTx only modestly affects cell proliferation, sustained treatment markedly reduces cell numbers, LeTx also substantially inhibits the extracellular release of angioproliferative factors including vascular endothelial growth factor, interleukin-8, and basic fibroblast growth factor, overview
-
AS-703026
-
a MEK1–2 inhibitor, binds in the allosteric site of MEK1. For A-375 cells, AS-703026 has a growth IC50 of 4 nM
-
AS703026
-
-
-
AZD8330
-
BAY 869766
-
i.e. RDEA119
-
Berberine
-
suppresses MEK/ERK-dependent Egr-1 signaling pathway and inhibits vascular smooth muscle cell regrowth after mechanical injury in vitro
capecitabine
-
-
CH-498755/RO498755
-
a MEK1/2 inhibitor
-
CH4987655
-
CI-1040
Cocoa procyanidin B2
-
procyanidin B2 suppresses TPA-induced phosphorylation of MEK, ERK, and p90RSK in JB6 P+ cells, suppresses JB6 P+ cell transformation by inhibiting mitogen-activated protein kinase kinase, molecular mechanism, overview
Cocoa procyanidins
-
suppresses JB6 P+ cell transformation by inhibiting mitogen-activated protein kinase kinase, molecular mechanisms of the chemopreventive potential of cocoa and its active ingredients, overview
-
E6201
-
blocks proliferation of many of the cell lines typically used in testing MEK inhibitors, such as Colo205 and MiaPaca-2
-
ethyl 4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylate
;
GDC0973
-
-
-
GSK1120212
-
-
-
LL-Z1640-2
-
a MEK1 inhibitor, which shows reasonable MEK inhibition but a very short half-life
-
MEK162
-
-
-
MIIC
-
i.e. MEK inhibitor I, the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption; i.e. MEK inhibitor I, the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption
-
N-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)-3,4-difluoro-5-hydroxybenzamide
-
-
N-(3-{3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)benzamide
-
-
N-(3-{3-cyclopropyl-5-[(4-cyclopropyl-2-fluorophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)-2-oxopropanamide
-
-
N-(3-{5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3-phenyl-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)-2-oxopropanamide
-
-
N-(3-{5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3-phenyl-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl}phenyl)benzamide
-
-
N-{3-[3-(3-fluoro-4-hydroxyphenyl)-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-2-oxopropanamide
-
-
N-{3-[5-(cyclopropylmethyl)-3-(3-fluoro-4-hydroxyphenyl)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-3,4-difluoro-5-hydroxybenzamide
-
-
N-{3-[5-(cyclopropylmethyl)-3-(4-hydroxy-3-iodophenyl)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-3,4-difluoro-5-hydroxybenzamide
-
-
N-{3-[5-(cyclopropylmethyl)-3-(4-hydroxyphenyl)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}-3,4-difluoro-5-hydroxybenzamide
-
-
PD0325901
-
-
-
PD098059
-
MEK1 inhibitor
PD184352
-
a MEK-specific inhibitor
PD184352/CI-1040
-
a allosteric, non-ATP competitive MEK inhibitor
-
PD198306
-
an orally active MEK1/2 inhibitor, acting as an uncoupler; an orally active MEK1/2 inhibitor, acting as an uncoupler
-
PD318088
PD98059
pemetrexed
-
-
phencyclidine
-
a N-methyl-D-aspartate receptor antagonist, it is neurotoxic to developing brains and results in schizophrenia-like behaviors later in development, it elicites time-dependent inhibition of the MEK/ERK and PI-3K/Akt pathways, overview
RDEA119
-
-
-
RDEA436
-
-
-
refametinib
-
-
-
RO4987655
-
-
-
RO5126766
-
-
-
selumetinib
-
siRNA
-
TAK733
-
-
-
temozolomide
-
-
tert-butyl [5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetate
-
trametinib
-
XL-518/GDC-0973
-
selective for MEK1 relative to MEK2
-
[5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetic acid
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
anisomycin
-
activates
CD40
-
activated by ligation of CD40, the B-cell antigen receptor
-
doxycycline
-
induces expression of HA-MEK1
growth factor interleukin-3
-
activates
-
additional information
-