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Information on EC 2.7.12.2 - mitogen-activated protein kinase kinase
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2.7.12.2 mitogen-activated protein kinase kinaseIUBMB Comments
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 . 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.
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Word Map
- 2.7.12.2
- mapks
- c-jun
- 3-kinase
- mek1
- pkc
- endothelial
- phosphatidylinositol
- agonist
- arrest
- necrosis
- metastasis
- raf-1
- camp
-
dominant-negative
- egf
- c-fos
- erk2
- nf-kappab
-
phorbol
- phosphoinositide
- caspase-3
-
stress-activated
- melanoma
- bcl-2
- cyclins
- rapamycin
- wortmannin
- pertussis
-
signal-related
- stat3
-
kinase-dependent
- mtor
- trametinib
-
brafv600e
-
egf-induced
- elk-1
-
p21ras
-
extracellular-regulated
-
ras-mediated
- phospho-erk
-
mek-erk
-
ras-dependent
- p38alpha
-
braf-mutant
-
erk-dependent
-
p90rsk
-
dual-specificity
- p38mapk
-
ras-induced
- medicine
- drug development
- rsk
- analysis
The enzyme appears in viruses and cellular organisms
Synonyms
apoptosis signal-regulating kinase 1, ASK1, At3g21220, BcOs4, BOS5, CaSTE7, cdc7 protein kinase, Cdc7p kinase, cell division control protein 7, cpkk1, 
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
ASK1
BcOs4
BOS5
dual specificity mitogen-activated protein kinase kinase 1
dual specificity mitogen-activated protein kinase kinase 2
dual specificity mitogen-activated protein kinase kinase 3
dual specificity mitogen-activated protein kinase kinase 4
dual specificity mitogen-activated protein kinase kinase 5
dual specificity mitogen-activated protein kinase kinase 6
dual specificity mitogen-activated protein kinase kinase 7
-
dual specificity mitogen-activated protein kinase kinase dSOR1
-
dual specificity mitogen-activated protein kinase kinase hemipterous
-
dual specificity mitogen-activated protein kinase kinase mek-2
-
ERK
extracellular signal-regulated kinase
extracellular-signal-regulated kinase
MAP kinase kinase
MAP kinase kinase 4
MAPK kinase
MAPK/Erk kinase
MAPKK
MAPKK1
MAPKK3
MEK
MEK-2
MEK1
MEK1/2
MEK2
MEK5
mitogen activated protein kinase kinase
mitogen activated protein kinase kinase 6
mitogen-activated protein kinase kinase
mitogen-activated protein kinase kinase 1
mitogen-activated protein kinase kinase 2
mitogen-activated protein kinase kinase 3
mitogen-activated protein kinase kinase 4
mitogen-activated protein kinase kinase kinase 2
mitogen-activated protein kinase kinase kinase 3
mitogen-activated protein kinase kinase kinase 5
mitogen-activated protein kinase kinase/extracellular signal–regulated kinase
-
-
mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1
-
mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 2
-
MKK
MKK1
MKK2
MKK3
MKK4
MKK5
MKK6
MKK7
OsMKK4
polymyxin B resistance protein kinase
-
serine/threonine protein kinase STE7
-
stress kinase mitogen-activated protein kinase kinase 7
stress-activate protein kinase/extracellular signal-regulated protein kinase kinase-1
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-
Tb927.10.5270
Tb927.3.4860
VdPbs2
additional information
dual specificity mitogen-activated protein kinase kinase 1
-
dual specificity mitogen-activated protein kinase kinase 1
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dual specificity mitogen-activated protein kinase kinase 1
-
dual specificity mitogen-activated protein kinase kinase 1
-
dual specificity mitogen-activated protein kinase kinase 2
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dual specificity mitogen-activated protein kinase kinase 2
-
dual specificity mitogen-activated protein kinase kinase 3
-
dual specificity mitogen-activated protein kinase kinase 4
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dual specificity mitogen-activated protein kinase kinase 6
-
mitogen activated protein kinase kinase
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
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-
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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.
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CAS REGISTRY NUMBER
COMMENTARY
142805-58-1
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + Erk-1 gene product
ADP + phosphorylated Erk-1 gene product
phosphorylation primarily on a tyrosine residue and, to a lesser extent, on a threonine
-
?
ATP + extracellular regulated kinase 1
ADP + phosphorylated extracellular regulated kinase 1
-
-
-
?
ATP + extracellular regulated kinase 2
ADP + phosphorylated extracellular regulated kinase 2
-
-
-
?
ATP + JNK
ADP + phopsho-JNK
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + K52R-[ERK2]
ADP + phospho-K52R-[ERK2]
-
catalytically inactive ERK2 in which lysine-52 is substituted with arginine
-
-
?
ATP + K53M-[p38alpha]
ADP + phospho-K53M-[p38alpha]
-
catalytically inactive p38alpha in which lysine-53 is substituted with methionine
-
-
?
ATP + MAP kinase 6
ADP + phosphorylated Map kinase 6
Arabidopsis thaliana MAP kinase MPK6
-
-
?
ATP + myelin basic protein
ADP + phoshorylated myelin basic protein
-
-
-
?
ATP + myelin basic protein kinase
ADP + phosphorylated myelin basic protein kinase
-
-
-
?
ATP + p38 MAP kinase
ADP + ?
-
phosphorylates and activates p38 MAP kinase
-
-
?
ATP + p38/MPK2 kinase
ADP + ?
-
phosphorylates and specifically activates the p38/MPK2 subgroup of the mitogen-activated protein kinase superfamily
-
-
?
ATP + p38alpha
ADP + phosphorylated p38alpha
-
MKK6 phosphorylates p38 MAPK on Thr180 and Tyr182, the sites of phosphorylation that activate p38 MAPK
-
-
?
ATP + Pfmap2
ADP + phosphorylated Pfmap2
-
the enzyme phosphorylates its potential in vivo Pfmap2 substrate largely on Thr290
-
-
?
ATP + poly-(Tyr-Glu)
ADP + phospho-poly-(Tyr-Glu)
-
tyrosine kinase substrate
-
-
?
ATP + [ERK2 substrate peptide]
ADP + [ERK2 substrate peptide] phosphate
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MEK1
-
-
?
ATP + [myelin basic protein substrate peptide]
ADP + [myelin basic protein substrate peptide] phosphate
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
MKK1 phosphorylates and activates the MAP kinases ERK1 and ERK2
-
-
?
ATP + BcSak1
ADP + phosphorylated BcSak1
protei BcSAK1 is the putative downstream component of BOS5
-
-
?
ATP + BcSak1
ADP + phosphorylated BcSak1
protei BcSAK1 is the putative downstream component of BOS5
-
-
?
ATP + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
-
JNK activation
-
-
?
ATP + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
-
JNK activation
-
-
?
ATP + ERK
ADP + phosphorylated ERK
-
phosphorylation by MEK activates ERK, which plays a role in pain induction modulating the A-type currents of potassium channels in neurons, ERK plays a central role in nocireceptive sensitization in the spinal cord
-
-
?
ATP + ERK1
ADP + phosphorylated ERK1
-
MEK2 protein stimulates Thr and Tyr phosphorylation on ERK1 and concomitantly activates ERK1 kinase activity more than 100-fold
-
-
?
ATP + ERK1
ADP + phosphorylated ERK1
-
phosphorylation of extracellular signal-regulated kinase 1
-
-
?
ATP + ERK2
ADP + phosphorylated ERK2
-
phosphorylation of extracellular signal-regulated kinase 2
-
-
?
ATP + ERK2
ADP + phosphorylated ERK2
-
MEK1 is able to effectively phosphorylate Thr183 and Tyr185 in the activation loop of ERK2
-
-
?
ATP + JNK
ADP + JNK phosphate
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + JNK
ADP + JNK phosphate
substrate of MKK4 and MKK7 in a synergistic manner
-
-
?
ATP + JNK
ADP + phospho-JNK
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
substrate of MKK4 and MKK7 in a synergistic manner
-
-
?
ATP + JNK
ADP + phospho-JNK
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
substrate of MKK4 and MKK7 in a synergistic manner
-
-
?
ATP + JNK
ADP + phospho-JNK
-
the enzyme is involved in stress-activated MAP kinase pathways and tumorigenesis, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
-
substrate of MKK4 and MKK7 in a synergistic manner
-
-
?
ATP + JNK
ADP + phosphorylated JNK
phosphorylation of JNK at the Thr residue located in the activation loop
-
-
?
ATP + JNK
ADP + phosphorylated JNK
phosphorylation of JNK at the Tyr residue located in the activation loop
-
-
?
ATP + JNK1
ADP + phosphorylated JNK1
-
slight phosphorylation, JNK1 may not be the optimal substrate for the isoform
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
activation of MAP kinase
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
the enzyme is involved in the mitogen-activated protein kinase signaling pathway important for e.g. flagellar length control, the enzyme is involved in differentiation of the parasite and is important for virulence and infection of human peritoneal macrophages
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
docking site for the substrate is located close to the N-terminal Lys4 and consists of 2 basic amino acid residues separated by a spacer of 2-6 variable residues from an L/I/V-X-L/I/V sequence
-
-
?
ATP + MPK-7
ADP + phospho-MPK-7
-
MKK3 interacts with MPK7 in planta
-
-
?
ATP + MPK-7
ADP + phospho-MPK-7
-
MKK3 interacts with MPK7 in planta
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
Pfnek3 phosphorylates MBP on threonine, but not serine residues
-
-
?
ATP + MyoD
ADP + phospharylated MyoD
-
phosphorylation at Tyr156, activated MEK1 associates with MyoD
-
-
?
ATP + MyoD
ADP + phospharylated MyoD
-
phosphorylation at Tyr156 recombinant GST-tagged MyoD substrate. Mutational analysis of phosphorylation sites using MyoD Tyr mutants, overview
-
-
?
ATP + p38
ADP + p38 phosphate
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + p38
ADP + phospho-p38
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + p38
ADP + phospho-p38
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + p38
ADP + phospho-p38
-
the enzyme is involved in stress-activated MAP kinase pathways and tumorigenesis, overview
-
-
?
ATP + p38
ADP + phospho-p38
signal cascade upstream activation by phosphorylation, sorbitol induced activation of p38 in salmon TO cells does not require MKK6a, b or c
-
-
?
ATP + protein
ADP + phosphoprotein
mek-2 acts between lin-45 raf and sur-1/mpk-1 in a signal transduction pathway used in the control of vulval differentiation and other developmental events
-
-
?
ATP + protein
ADP + phosphoprotein
Hst7 activates the mating pathway even in the absence of upstream signaling components including the Ste7 regulator Ste11, elevates the basal level of the pheromone-inducible FUS1 gene, and amplifies the pseudohyphal growth response in diploid cells
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme functions in a novel Drosophila MAPK pathway, controlling puckered expression and morphogenetic activity of the dorsal epidermis
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme is involved in the mitogenic growth factor signal transduction pathway in vertebrates
-
-
?
ATP + protein
ADP + phosphoprotein
enzyme is involved in independent human MAP-kinase signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
MKK4 may participate in a tumor suppressive signaling pathway distinct from DPC4, p16, p53, and BRCA2. The enzyme is a component of a stress and cytokine-induced signal transduction pathway involving MAPK proteins, additional role for MKK4 in tumor suppression
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme is an activator of the c-Jun NH2-terminal kinase, the enzyme is a component of the JNK signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is the major activator for p38
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is involved on MAPK signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme is the major activator of RK/p38
-
-
?
ATP + protein
ADP + phosphoprotein
MEKK3 regulates the SAPK and the ERK pathway directly
-
-
?
ATP + protein
ADP + phosphoprotein
-
ASK1 may be a key element in the mechanism of stress-induced and cytokine-induced apoptosis
-
-
?
ATP + protein
ADP + phosphoprotein
-
MEK6 is a member of the p38 kinase cascade and efficiently phosphorylates p38, induces phosphorylation of ATF2 by p38 but does not phosphorylate ATF2 directly
-
-
?
ATP + protein
ADP + phosphoprotein
-
MAPKKK5 may be an upstream activator of MKK4 in the c-Jun N-terminal kinase pathway
-
-
?
ATP + protein
ADP + phosphoprotein
sequences located in the N-terminus of MEK5 may be important in coupling GTPase signaling molecules to the MEK5 protein kinase cascade
-
-
-
ATP + protein
ADP + phosphoprotein
phosphorylates kinase-inactive Erk-1 protein primarily on a tyrosine residue and, to a lesser extent, on a threonine
-
-
?
ATP + protein
ADP + phosphoprotein
possible role for ASK1 in tissue development during embryogenesis as well as cytokine-induced apoptosis
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is the major activator for p38
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is involved on MAPK signal transduction pathway
-
-
-
ATP + protein
ADP + phosphoprotein
MEKK 2 preferentially activates JNK
-
-
?
ATP + protein
ADP + phosphoprotein
MEKK 3 preferentially activates p42/44MAPK
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme renders the cell resistant to polymyxin B
-
-
?
ATP + protein
ADP + phosphoprotein
-
MKK1 and MKK2 function in a signal transduction pathway involving the protein kinases encoded by PKC1, BCK1, and MPK1. The site of action for MKK1 and MKK2 is between BCK1 and MPK1
-
-
?
ATP + protein
ADP + phosphoprotein
enzyme is involved in the response of haploid yeast cells to peptide mating pheromones
-
-
?
ATP + protein
ADP + phosphoprotein
-
Pek1, in its unphosphorylated form, acts as a potent negative regulator of Pmk1 MAPK signalling. Mkh1, an upstream MAPKK kinase, converts Pek1 from being an inhibitor to an activator. Pek1 has a dual stimulatory and inhibitory function which depends on its phosphorylation state
-
-
?
ATP + protein
ADP + phosphoprotein
enzyme plays a key role in initiation of septum formation and cytokinesis in fission yeast, p120cdc7 interacts with the cdc11 protein in the control of septation
-
-
?
ATP + protein
ADP + phosphoprotein
-
dosage-dependent regulator of mitosis in Schizosaccharomyces pombe
-
-
?
ATP + protein
ADP + phosphoprotein
-
Spg1p is a key element in controlling the onset of septum formation that acts through the Cdc7p kinase
-
-
?
ATP + protein
ADP + phosphoprotein
-
byr1 is an important gene in the sexual differentiation pathway and at least part of ras1 function is to act directly or indirectly through byr1 to modulate protein phosphorylation
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme is a component of the mkh1 signaling pathway. Mkh1, Skh1 and Spm1 constitute a MAPK cascade in Schizosaccharomyces pombe
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme is required for locus-dependent and locus-independent steps in the fungal life cycle. Necessary for locus-dependent processes, such as conjugation tube formation, filament formation, and maintenance of filamentous growth, and for locus-independent processes, such as tumor induction and teliospore germination
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme undergoes autophosphorylation on Ser, Thr and Tyr
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme functions as a direct upstream activator for a presumed MAP kinase homolog in each signal transduction pathway involved in the regulation of cell cycle progression or cellular responses to extracellular signals
-
-
?
ATP + Smad3
ADP + phosphorylated Smad3
-
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
-
VdHog1 is a mitogen-activated protein kinase, MAPK
-
-
?
ATP + VdHog1
ADP + phosphorylated VdHog1
-
VdHog1 is a mitogen-activated protein kinase, MAPK
-
-
?
additional information
?
-
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK1 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. The mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK1 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. The mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
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Arabidopsis thaliana mitogen-activated protein kinase kinase MKK2 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. mkk2 single mutants appear morphologically normal, the mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK2 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. mkk2 single mutants appear morphologically normal, the mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
-
MKK3 positively regulates PR gene expression and plays a role in defense against Pst DC3000. MKK3 is an upstream activator of the group C MAPKs MPK1, MPK2, MPK7, and MPK14, overview
-
-
-
additional information
?
-
-
MKK3 positively regulates PR gene expression and plays a role in defense against Pst DC3000. MKK3 is an upstream activator of the group C MAPKs MPK1, MPK2, MPK7, and MPK14, overview
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-
-
additional information
?
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-
substrate binding via the D-domain of the MKK
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-
additional information
?
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enzyme is part of mitogen-activated protein kinase pathways, crosstalk and regulation mechanism, overview
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additional information
?
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GhMKK3 interacts with GhMPK7, a typical C group MAPK member, and GhPIP1 potein. GhMPK7 is phosphorylated by GhMKK3 in protoplasts
-
-
-
additional information
?
-
S4S5K3
GhMKK3 interacts with GhMPK7, a typical C group MAPK member, and GhPIP1 potein. GhMPK7 is phosphorylated by GhMKK3 in protoplasts
-
-
-
additional information
?
-
MEKK3 activates SEK and MEK, the known kinases targeting SAPK and ERK respectively
-
-
-
additional information
?
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-
MEK1/2 are involved in the mitogen-activated protein kinase signaling pathway and in cancer tumorigenesis
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-
-
additional information
?
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the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is linked to the cell cycle machinery, constitutive phosphorylation and activation of the enzyme leads to cell proliferation in choroidal melanoma cells
-
-
-
additional information
?
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-
mitogen-activated protein kinase kinase signaling promotes growth and vascularization of fibrosarcoma it is required for growth of fibrosarcoma-derived xenografts, to maintain tumor blood flow, and for vascularization of fibrosarcoma-derived xenografts, and MKK signaling is required for the release of proangiogenic factors from other sarcoma-derived cell lines, overview
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-
-
additional information
?
-
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview
-
-
-
additional information
?
-
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview
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-
-
additional information
?
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-
the MEKK-1 is involved in stress-induced cell death of insulin-producing cells and essential in JNK activation, overview
-
-
-
additional information
?
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-
TNF-alpha receptor signaling regulates epithelial cell secretion of inflammation and invasion mediators involving signaling through IkappaB kinase complex 2, IKB, nuclear factor kappaB, extracellular signal-regulated kinase, mitogen-activated protein kinase kinase, p38, and phosphatidylinositol 3-kinase, and Akt1/2. MEK, p38, and IKK inhibitors block TNF-alpha-induced IL-8, IL-6, and GM-CSF secretion and 12z invasion, whereas the PI3K inhibitors do not, overview
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-
-
additional information
?
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-
MKK signaling is required for cell proliferation and for cytokine release in vitro
-
-
-
additional information
?
-
substrate binding via the D-domain of the MKK
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-
-
additional information
?
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substrate binding via the D-domain of the MKK
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-
-
additional information
?
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-
development of a continuous spectrophotometric assay for mitogen-activated protein kinase kinases. The assay relies on the measurement of phosphoprotein product generated in the first step of the MAPK kinase reaction. Dephosphorylation of the phosphoprotein is coupled to a MAPK phosphatase, MKP3, to generate phosphate, which is then used as the substrate of purine nucleoside phosphorylase to catalyze the N-glycosidic cleavage of 2-amino 6-mercapto 7-methyl purine ribonucleoside. Of the reaction products ribose 1-phosphate and 2-amino 6-mercapto 7-methylpurine, the latter has a high absorbance at 360 nm relative to the nucleoside and, hence, provides a spectrophotometric signal that can be continuously followed. In the presence of excess phosphatase, the phosphorylated protein substrate molecules undergo dephosphorylation almost immediately after their formation. The steady-state use of the resultant inorganic phosphate is a reflection of the constant initial velocity of the exchange reaction. Method development and evaluation, overview
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-
-
additional information
?
-
-
development of a continuous spectrophotometric assay for mitogen-activated protein kinase kinases. The assay relies on the measurement of phosphoprotein product generated in the first step of the MAPK kinase reaction. Dephosphorylation of the phosphoprotein is coupled to a MAPK phosphatase, MKP5, to generate phosphate, which is then used as the substrate of purine nucleoside phosphorylase to catalyze the N-glycosidic cleavage of 2-amino 6-mercapto 7-methyl purine ribonucleoside. Of the reaction products ribose 1-phosphate and 2-amino 6-mercapto 7-methylpurine, the latter has a high absorbance at 360 nm relative to the nucleoside and, hence, provides a spectrophotometric signal that can be continuously followed. In the presence of excess phosphatase, the phosphorylated protein substrate molecules undergo dephosphorylation almost immediately after their formation. The steady-state use of the resultant inorganic phosphate is a reflection of the constant initial velocity of the exchange reaction. Method development and evaluation, overview
-
-
-
additional information
?
-
-
the enzyme performs autophosphorylation
-
-
-
additional information
?
-
the enzyme performs autophosphorylation
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway regulating cell dissociation of cancer cells, MEK2 is an invasion-metastasis related factor between highly and weakly invasive cells, occludin acts as antagonist
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is involved in e.g. formalin-induced inflammatory pain and thermal hyperalgesia, overview
-
-
-
additional information
?
-
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
additional information
?
-
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
additional information
?
-
substrate binding via the D-domain of the MKK
-
-
-
additional information
?
-
substrate binding via the D-domain of the MKK
-
-
-
additional information
?
-
MKK4 phosphorylates JNK on Tyr, while MKK7 phosphorylates Thr, and MKK4 and MKK7 together cause dual phosphorylation of JNK thus, optimal activation
-
-
-
additional information
?
-
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
regulation and differential expression, overview
-
-
-
additional information
?
-
regulation and differential expression, overview
-
-
-
additional information
?
-
regulation and differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
regulation and differential expression, overview
-
-
-
additional information
?
-
regulation and differential expression, overview
-
-
-
additional information
?
-
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
-
the enzyme displays both serine/threonine and tyrosine kinase activities in autophosphorylation reactions as well as in phosphorylation of the exogenous myelin basic protein substrate. Ability of Pfnek3 to autophosphorylate on both the serine/threonine and the tyrosine residues. The dual-specificity activity of the kinase is distinctly influenced by the type of divalent cation present
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, pathway induction by neurotrophin stabilizes the axonal growth cone, pathway inhibitor semaphorin 3F induces growth cone collaps in sympathetic neurons and reduction of axonal growth
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is involved in e.g. activation of Egr-1 and subsequently of c-Fos and cyclin D1 after mechanic injury for induction/regulation of regrowth of smooth vascular cells, vascular smooth muscle cell proliferation plays an important role in pathogenesis of atherosclerosis and post-angioplasty restenosis, overview
-
-
-
additional information
?
-
-
adenosine-stimulated adrenal steroidogenesis involves the adenosine A2A and A2B receptors and the Janus kinase 2-mitogen-activated protein kinase kinase-extracellular signal-regulated kinase signaling pathway, overview
-
-
-
additional information
?
-
-
lithium protection of phencyclidine-induced neurotoxicity and cell death in developing brain: the role of phosphatidylinositol-3 kinase/Akt and mitogen-activated protein kinase kinase/extracellular signal-regulated kinase signaling pathways, overview
-
-
-
additional information
?
-
-
role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
additional information
?
-
-
substrate binding via the D-domain of the MKK
-
-
-
additional information
?
-
-
Pek1, in its unphosphorylated form, acts as a potent negative regulator of Pmk1 MAPK signalling. Mkh1, an upstream MAPKK kinase, converts Pek1 from being an inhibitor to an activator. Pek1 has a dual stimulatory and inhibitory function which depends on its phosphorylation state
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-
-
additional information
?
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-
substrate binding via the D-domain of the MKK
-
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
ATP + ERK1
ADP + phosphorylated ERK1
-
phosphorylation of extracellular signal-regulated kinase 1
-
-
?
ATP + extracellular regulated kinase 1
ADP + phosphorylated extracellular regulated kinase 1
I3L5D4
-
-
-
?
ATP + extracellular regulated kinase 2
ADP + phosphorylated extracellular regulated kinase 2
I3L5D4
-
-
-
?
ATP + JNK
ADP + JNK phosphate
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + JNK
ADP + phopsho-JNK
P47809, Q8CE90
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
Pfnek3 phosphorylates MBP on threonine, but not serine residues
-
-
?
ATP + MyoD
ADP + phospharylated MyoD
-
phosphorylation at Tyr156, activated MEK1 associates with MyoD
-
-
?
ATP + p38
ADP + p38 phosphate
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + p38alpha
ADP + phosphorylated p38alpha
-
MKK6 phosphorylates p38 MAPK on Thr180 and Tyr182, the sites of phosphorylation that activate p38 MAPK
-
-
?
ATP + Pfmap2
ADP + phosphorylated Pfmap2
-
the enzyme phosphorylates its potential in vivo Pfmap2 substrate largely on Thr290
-
-
?
ATP + Smad3
ADP + phosphorylated Smad3
-
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 + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
-
JNK activation
-
-
?
ATP + c-Jun N-terminal kinase
ADP + phosphorylated c-Jun N-terminal kinase
-
JNK activation
-
-
?
ATP + ERK
ADP + phosphorylated ERK
-
phosphorylation by MEK activates ERK, which plays a role in pain induction modulating the A-type currents of potassium channels in neurons, ERK plays a central role in nocireceptive sensitization in the spinal cord
-
-
?
ATP + ERK2
ADP + phosphorylated ERK2
-
phosphorylation of extracellular signal-regulated kinase 2
-
-
?
ATP + JNK
ADP + phospho-JNK
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + JNK
ADP + phospho-JNK
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
-
the enzyme is involved in stress-activated MAP kinase pathways and tumorigenesis, overview
-
-
?
ATP + JNK
ADP + phosphorylated JNK
Q8CE90
phosphorylation of JNK at the Thr residue located in the activation loop
-
-
?
ATP + JNK
ADP + phosphorylated JNK
Q8CE90
phosphorylation of JNK at the Tyr residue located in the activation loop
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
O80396
activation of MAP kinase
-
-
?
ATP + MAP kinase
ADP + phosphorylated MAP kinase
Q9GRT1
the enzyme is involved in the mitogen-activated protein kinase signaling pathway important for e.g. flagellar length control, the enzyme is involved in differentiation of the parasite and is important for virulence and infection of human peritoneal macrophages
-
-
?
ATP + MPK-7
ADP + phospho-MPK-7
-
MKK3 interacts with MPK7 in planta
-
-
?
ATP + MPK-7
ADP + phospho-MPK-7
-
MKK3 interacts with MPK7 in planta
-
-
?
ATP + p38
ADP + phospho-p38
O14733, P45985
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer, physiologic effects, overview
-
-
?
ATP + p38
ADP + phospho-p38
P47809, Q8CE90
the enzyme is involved in stress-activated MAP kinase pathways, tumorigenesis, and cancer acting as a metastasis suppressor, overview
-
-
?
ATP + p38
ADP + phospho-p38
-
the enzyme is involved in stress-activated MAP kinase pathways and tumorigenesis, overview
-
-
?
ATP + p38
ADP + phospho-p38
A9UK00
signal cascade upstream activation by phosphorylation, sorbitol induced activation of p38 in salmon TO cells does not require MKK6a, b or c
-
-
?
ATP + protein
ADP + phosphoprotein
Q10664
mek-2 acts between lin-45 raf and sur-1/mpk-1 in a signal transduction pathway used in the control of vulval differentiation and other developmental events
-
-
?
ATP + protein
ADP + phosphoprotein
P0CY25
Hst7 activates the mating pathway even in the absence of upstream signaling components including the Ste7 regulator Ste11, elevates the basal level of the pheromone-inducible FUS1 gene, and amplifies the pseudohyphal growth response in diploid cells
-
-
?
ATP + protein
ADP + phosphoprotein
Q23977
the enzyme functions in a novel Drosophila MAPK pathway, controlling puckered expression and morphogenetic activity of the dorsal epidermis
-
-
?
ATP + protein
ADP + phosphoprotein
Q90891
the enzyme is involved in the mitogenic growth factor signal transduction pathway in vertebrates
-
-
?
ATP + protein
ADP + phosphoprotein
P45985, P46734
enzyme is involved in independent human MAP-kinase signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
MKK4 may participate in a tumor suppressive signaling pathway distinct from DPC4, p16, p53, and BRCA2. The enzyme is a component of a stress and cytokine-induced signal transduction pathway involving MAPK proteins, additional role for MKK4 in tumor suppression
-
-
?
ATP + protein
ADP + phosphoprotein
O14733
the enzyme is an activator of the c-Jun NH2-terminal kinase, the enzyme is a component of the JNK signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is the major activator for p38
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is involved on MAPK signal transduction pathway
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme is the major activator of RK/p38
-
-
?
ATP + protein
ADP + phosphoprotein
Q99759
MEKK3 regulates the SAPK and the ERK pathway directly
-
-
?
ATP + protein
ADP + phosphoprotein
-
ASK1 may be a key element in the mechanism of stress-induced and cytokine-induced apoptosis
-
-
?
ATP + protein
ADP + phosphoprotein
-
MEK6 is a member of the p38 kinase cascade and efficiently phosphorylates p38, induces phosphorylation of ATF2 by p38 but does not phosphorylate ATF2 directly
-
-
?
ATP + protein
ADP + phosphoprotein
-
MAPKKK5 may be an upstream activator of MKK4 in the c-Jun N-terminal kinase pathway
-
-
?
ATP + protein
ADP + phosphoprotein
Q13163
sequences located in the N-terminus of MEK5 may be important in coupling GTPase signaling molecules to the MEK5 protein kinase cascade
-
-
-
ATP + protein
ADP + phosphoprotein
O35099
possible role for ASK1 in tissue development during embryogenesis as well as cytokine-induced apoptosis
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is the major activator for p38
-
-
?
ATP + protein
ADP + phosphoprotein
-
enzyme is involved on MAPK signal transduction pathway
-
-
-
ATP + protein
ADP + phosphoprotein
Q61083, Q61084
MEKK 2 preferentially activates JNK
-
-
?
ATP + protein
ADP + phosphoprotein
Q61083, Q61084
MEKK 3 preferentially activates p42/44MAPK
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme renders the cell resistant to polymyxin B
-
-
?
ATP + protein
ADP + phosphoprotein
-
MKK1 and MKK2 function in a signal transduction pathway involving the protein kinases encoded by PKC1, BCK1, and MPK1. The site of action for MKK1 and MKK2 is between BCK1 and MPK1
-
-
?
ATP + protein
ADP + phosphoprotein
P06784
enzyme is involved in the response of haploid yeast cells to peptide mating pheromones
-
-
?
ATP + protein
ADP + phosphoprotein
-
Pek1, in its unphosphorylated form, acts as a potent negative regulator of Pmk1 MAPK signalling. Mkh1, an upstream MAPKK kinase, converts Pek1 from being an inhibitor to an activator. Pek1 has a dual stimulatory and inhibitory function which depends on its phosphorylation state
-
-
?
ATP + protein
ADP + phosphoprotein
P41892
enzyme plays a key role in initiation of septum formation and cytokinesis in fission yeast, p120cdc7 interacts with the cdc11 protein in the control of septation
-
-
?
ATP + protein
ADP + phosphoprotein
-
dosage-dependent regulator of mitosis in Schizosaccharomyces pombe
-
-
?
ATP + protein
ADP + phosphoprotein
-
Spg1p is a key element in controlling the onset of septum formation that acts through the Cdc7p kinase
-
-
?
ATP + protein
ADP + phosphoprotein
-
byr1 is an important gene in the sexual differentiation pathway and at least part of ras1 function is to act directly or indirectly through byr1 to modulate protein phosphorylation
-
-
?
ATP + protein
ADP + phosphoprotein
-
the enzyme is a component of the mkh1 signaling pathway. Mkh1, Skh1 and Spm1 constitute a MAPK cascade in Schizosaccharomyces pombe
-
-
?
ATP + protein
ADP + phosphoprotein
Q99078
the enzyme is required for locus-dependent and locus-independent steps in the fungal life cycle. Necessary for locus-dependent processes, such as conjugation tube formation, filament formation, and maintenance of filamentous growth, and for locus-independent processes, such as tumor induction and teliospore germination
-
-
?
ATP + protein
ADP + phosphoprotein
Q05116
the enzyme functions as a direct upstream activator for a presumed MAP kinase homolog in each signal transduction pathway involved in the regulation of cell cycle progression or cellular responses to extracellular signals
-
-
?
ATP + VdHog1
ADP + phosphorylated VdHog1
-
VdHog1 is a mitogen-activated protein kinase, MAPK
-
-
?
ATP + VdHog1
ADP + phosphorylated VdHog1
-
VdHog1 is a mitogen-activated protein kinase, MAPK
-
-
?
additional information
?
-
Q94A06
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK1 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. The mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
Q9S7U9
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK1 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. The mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
Q94A06
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK2 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. mkk2 single mutants appear morphologically normal, the mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
Q9S7U9
Arabidopsis thaliana mitogen-activated protein kinase kinase MKK2 is implicated in biotic and abiotic stress responses as part of a signaling cascade including MEKK1 and MPK4, MKK1 and MKK2 function upstream of MPK4, overview. mkk2 single mutants appear morphologically normal, the mkk1/2 double mutant is similar to the mpk4 mutant, as both: (1) are dark green dwarves with curled leaves, (2) constitutively overproduce salicylic acid and exhibit enhanced resistance to biotrophic pathogens and insensitivity to JA, and (3) have enhanced basal expression of PR1 and other SA-dependent defense genes
-
-
-
additional information
?
-
-
MKK3 positively regulates PR gene expression and plays a role in defense against Pst DC3000. MKK3 is an upstream activator of the group C MAPKs MPK1, MPK2, MPK7, and MPK14, overview
-
-
-
additional information
?
-
-
MKK3 positively regulates PR gene expression and plays a role in defense against Pst DC3000. MKK3 is an upstream activator of the group C MAPKs MPK1, MPK2, MPK7, and MPK14, overview
-
-
-
additional information
?
-
-
enzyme is part of mitogen-activated protein kinase pathways, crosstalk and regulation mechanism, overview
-
-
-
additional information
?
-
-
GhMKK3 interacts with GhMPK7, a typical C group MAPK member, and GhPIP1 potein. GhMPK7 is phosphorylated by GhMKK3 in protoplasts
-
-
-
additional information
?
-
S4S5K3
GhMKK3 interacts with GhMPK7, a typical C group MAPK member, and GhPIP1 potein. GhMPK7 is phosphorylated by GhMKK3 in protoplasts
-
-
-
additional information
?
-
-
MEK1/2 are involved in the mitogen-activated protein kinase signaling pathway and in cancer tumorigenesis
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is linked to the cell cycle machinery, constitutive phosphorylation and activation of the enzyme leads to cell proliferation in choroidal melanoma cells
-
-
-
additional information
?
-
-
mitogen-activated protein kinase kinase signaling promotes growth and vascularization of fibrosarcoma it is required for growth of fibrosarcoma-derived xenografts, to maintain tumor blood flow, and for vascularization of fibrosarcoma-derived xenografts, and MKK signaling is required for the release of proangiogenic factors from other sarcoma-derived cell lines, overview
-
-
-
additional information
?
-
O14733
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview
-
-
-
additional information
?
-
P45985
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview
-
-
-
additional information
?
-
-
the MEKK-1 is involved in stress-induced cell death of insulin-producing cells and essential in JNK activation, overview
-
-
-
additional information
?
-
-
TNF-alpha receptor signaling regulates epithelial cell secretion of inflammation and invasion mediators involving signaling through IkappaB kinase complex 2, IKB, nuclear factor kappaB, extracellular signal-regulated kinase, mitogen-activated protein kinase kinase, p38, and phosphatidylinositol 3-kinase, and Akt1/2. MEK, p38, and IKK inhibitors block TNF-alpha-induced IL-8, IL-6, and GM-CSF secretion and 12z invasion, whereas the PI3K inhibitors do not, overview
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway regulating cell dissociation of cancer cells, MEK2 is an invasion-metastasis related factor between highly and weakly invasive cells, occludin acts as antagonist
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is involved in e.g. formalin-induced inflammatory pain and thermal hyperalgesia, overview
-
-
-
additional information
?
-
P47809
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
additional information
?
-
Q8CE90
pro-oncogenic role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
additional information
?
-
Q8CE90
MKK4 phosphorylates JNK on Tyr, while MKK7 phosphorylates Thr, and MKK4 and MKK7 together cause dual phosphorylation of JNK thus, optimal activation
-
-
-
additional information
?
-
A2XE35
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
A3FK65
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
Q0MSI2
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
Q5QN75
MAP kinase kinase 1 is regulated by salt and drought stresses, differential expression, overview
-
-
-
additional information
?
-
A2XE35
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
A3FK65
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
Q0MSI2
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
Q5QN75
MAP kinase kinase 10-2 is regulated only by cold stress, differential expression, overview
-
-
-
additional information
?
-
A2XE35
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
A3FK65
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0MSI2
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q5QN75
MAP kinase kinase 6 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
A2XE35
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
A3FK65
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0MSI2
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
Q5QN75
MAP kinase kinases 4 is strongly regulated by cold and salt stresses, differential expression, overview
-
-
-
additional information
?
-
A2XE35
regulation and differential expression, overview
-
-
-
additional information
?
-
A3FK65
regulation and differential expression, overview
-
-
-
additional information
?
-
Q0MSI2
regulation and differential expression, overview
-
-
-
additional information
?
-
Q0Z7Z4
regulation and differential expression, overview
-
-
-
additional information
?
-
Q5QN75
regulation and differential expression, overview
-
-
-
additional information
?
-
A2XE35
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
A3FK65
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
A5A544
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
I3RJI6
protein-protein docking of MAPKK and MAPK
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, pathway induction by neurotrophin stabilizes the axonal growth cone, pathway inhibitor semaphorin 3F induces growth cone collaps in sympathetic neurons and reduction of axonal growth
-
-
-
additional information
?
-
-
the enzyme is involved in the mitogen-activated protein kinase signaling pathway, which is involved in e.g. activation of Egr-1 and subsequently of c-Fos and cyclin D1 after mechanic injury for induction/regulation of regrowth of smooth vascular cells, vascular smooth muscle cell proliferation plays an important role in pathogenesis of atherosclerosis and post-angioplasty restenosis, overview
-
-
-
additional information
?
-
-
adenosine-stimulated adrenal steroidogenesis involves the adenosine A2A and A2B receptors and the Janus kinase 2-mitogen-activated protein kinase kinase-extracellular signal-regulated kinase signaling pathway, overview
-
-
-
additional information
?
-
-
lithium protection of phencyclidine-induced neurotoxicity and cell death in developing brain: the role of phosphatidylinositol-3 kinase/Akt and mitogen-activated protein kinase kinase/extracellular signal-regulated kinase signaling pathways, overview
-
-
-
additional information
?
-
-
role of mitogen-activated protein kinase kinase 4 in cancer, overview. MKK4 is also involved in the immune system and development of B- and T-cells, as well as in cardiac hypertrophy, overview
-
-
-
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
ATP
subdomain II with an invariable lysine residue is responsible for ATP binding
ATP
-
upon ATP-binding, the transient conformation adopted the configuration of typical kinase folding. In the absence of ATP-binding, the transient state of apo npMAP2K4 may shift to a state of aggregation via non-particular hydrophobic interactions as a result of the exposed hydrophobic residues
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Ca2+
-
elevation of cytosolic Ca2+ by ethylene may stimulate protein phosphatase and MAPKK, which finally activates IPO expression
Mg2+
Mn2+
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
Mg2+
-
dependent on, Mg2+ is the physiologic metal ion, other divalent cations are able to support nucleotide binding, but only Mn2+, Co2+, and Cd2+ can substitute Mg2+ in supporting the catalytic activity
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
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-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
Berberine
-
suppresses MEK/ERK-dependent Egr-1 signaling pathway and inhibits vascular smooth muscle cell regrowth after mechanical injury in vitro
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
;
LL-Z1640-2
-
a MEK1 inhibitor, which shows reasonable MEK inhibition but a very short half-life
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
-
-
PD198306
-
an orally active MEK1/2 inhibitor, acting as an uncoupler; an orally active MEK1/2 inhibitor, acting as an uncoupler
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
tert-butyl [5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetate
-
[5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetic acid
-
CH4987655
-
or RO4987655, a non-ATP competitive inhibitor, highly selective for MEK1
PD98059
-
MEK-specific inhibitor, enhances antileukemia activity of Mdm2 antagonists in AML cells and p53-mediated transcription-dependent apoptosis. MEK inhibition accumulates p53 into the nucleus in OCIAML-3 cells, but does not affect the nucleoplasmic localization of Mdm2. The inhibitor restricts p21-mediated antiapoptotic mechanisms by repressing p53-dependent induction of p21, which enables Nutlin-3a to induce sufficient apoptosis in G1-phase cells
PD98059
-
inhibition of MEK1 with either PD98059 results in a substantial dose-dependent inhibition of SMAD3 promoter activity, reduced SMAD3 protein expression in A549 cells and airway smooth muscle cells after treatment with MEK1 inhibitors; substantial dose-dependent inhibition of SMAD3 promoter activity, 5.8fold reduction, MEK1 inhibition of SMAD3 promoter function is primarily mediated through an Sp1-dependent mechanism
PD98059
-
the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption; the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption
PD98059
-
MAPKK inhibitor, inhibits IPO expression stimulated by staurosporine
PD98059
-
inhibitor specific for MEK/ERK activation, granulocyte/macrophage colony number is decreased by ca. 60%
PD98059
-
the MEK inhibitor completely blocks adenosine-stimulated corticosterone production
selumetinib
-
i.e. AZD6244, potent and highly selective, non-ATP competitive inhibitor of MEK1/2, MEK1 phosphorylation of ERK2. The compound inhibits growth of cell lines
siRNA
-
MEK1/2-specific inhibitor, delays, but does not block the passage of synchronized HeLa cells into M phase
-
siRNA
-
cells transiently transfected with two independent sets of siRNAs show significant down-regulation of MKK3 and phosphorylated MKK3
-
siRNA
-
knockdown of MEK, HSCs give rise to Mac-1+ myeloid cells less efficiently than control HSCs
-
trametinib
a mitogen-activated protein kinase kinase 1 (MEK1)/MEK2 inhibitor with activity against multiple myeloid cell lines at low nanomolar concentrations, preferential activity among RAS-mutated myeloid malignancies. During clinical oral treatment, most commonly reported treatment-related adverse events are diarrhea, rash, nausea, and increased alanine aminotransferase levels, repeated cycles of trametinib are well tolerated with manageable or reversible toxicities, overview; a mitogen-activated protein kinase kinase 1 (MEK1)/MEK2 inhibitor with activity against multiple myeloid cell lines at low nanomolar concentrations, preferential activity among RAS-mutated myeloid malignancies. During clinical oral treatment, most commonly reported treatment-related adverse events are diarrhea, rash, nausea, and increased alanine aminotransferase levels, repeated cycles of trametinib are well tolerated with manageable or reversible toxicities, overview
U0126
-
inhibition of MEK1 with either UO126 results in a substantial dose-dependent inhibition of SMAD3 promoter activity, reduced SMAD3 protein expression in A549 cells and airway smooth muscle cells after treatment with MEK1 inhibitors; substantial dose-dependent inhibition of SMAD3 promoter activity, 2.3fold reduction, MEK1 inhibition of SMAD3 promoter function is primarily mediated through an Sp1-dependent mechanism
U0126
-
MEK1/2-specific inhibitor, delays, but does not block the passage of synchronized HeLa cells into M phase
U0126
-
the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption; the MEK1/2 inhibitor causes NAD(H) reduction, heme oxidation, and decreased oxygen consumption
U0126
-
inhibitor specific for MEK/ERK activation, granulocyte/macrophage colony number is decreased by ca. 60%
U0126
-
potent MEK-1/2 inhibitor, cellular size, DNA fragmentation, nuclear condensation, and the phosphorylated ERK-1 protein products of H9c2 cells treated with Porphyromonas gingivalis medium, are all significantly reduced after pre-administration of U0126
U0126
-
the MEK inhibitor completely blocks adenosine-stimulated corticosterone production
additional information
-
MEK, p38, and IKK inhibitors block TNF-alpha-induced IL-8, IL-6, and GM-CSF secretion and 12z invasion, whereas the PI3K inhibitors do not
-
additional information
-
stress-induced target of rapamycin complex 1 activation can be blocked by RNAi against mitogen-activated protein kinase kinase 3 and 6
-
additional information
-
known inhibitor structure screening, and design of specific allosteric MEK1/2 inhibitors with improved pharmacokinetic/pharmacodynamic profiles to be used as alternative cancer medications. Trametinib is used as the lead structure. Molecular docking and binding simulations, thermodynamics, and quantitative structure-activity relationships, allosteric inhibitory site, overview
-
additional information
-
the MEK enzyme contains a hydrophobic allosteric pocket adjacent to the ATP-binding site which allows for the design of highly selective allosteric inhibitors
-
additional information
-
design of small molecule MEK1/2 inhibitors to block ERK1/2-mediated signaling and inhibit proliferation. Four structurally distinct MEK1/2 inhibitors acutely affect mitochondrial bioenergetics. The anti-mitochondrial effects of MEK1/2 inhibitors determine the proliferative potential; design of small molecule MEK1/2 inhibitors to block ERK1/2-mediated signaling and inhibit proliferation. Four structurally distinct MEK1/2 inhibitors acutely affect mitochondrial bioenergetics. The anti-mitochondrial effects of MEK1/2 inhibitors determine the proliferative potential
-
additional information
SymRK acts as an inhibitor of SIP2 kinase activity when MPK6 is used as a substrate, suggesting that SymRK may serve as a negative regulator of the SIP2 signaling pathway. SymRK and SIP2 interact with each other but cannot use one another as a substrate for phosphorylation. SymRK can autophosphorylate itself but fails to phosphorylate the kinase-negative SIP2-KR, suggesting that SymRK is neither a potential phosphorylation target nor a kinase source of SIP2
-
additional information
-
SymRK acts as an inhibitor of SIP2 kinase activity when MPK6 is used as a substrate, suggesting that SymRK may serve as a negative regulator of the SIP2 signaling pathway. SymRK and SIP2 interact with each other but cannot use one another as a substrate for phosphorylation. SymRK can autophosphorylate itself but fails to phosphorylate the kinase-negative SIP2-KR, suggesting that SymRK is neither a potential phosphorylation target nor a kinase source of SIP2
-
additional information
-
occludin acts as antagonist of the MEK and ERK signaling pathway inducing cell aggregation of pancreatic cancer cells
-
additional information
-
inactivated by the serine/threonine phosphatase 2A but not by the protein-tyrosine phosphatase 1B
-
additional information
-
treatment with LY294002, paclitaxel, or serum starvation does not induce apoptosis of wild-type MEF cells
-
additional information
design and synthesis of 4-anilino-5-carboxamido-2-pyridone MEK1 inhibitors using a combination of medicinal chemistry, computational chemistry, and structural elucidation, overview. Binding structure analysis, overview
-
additional information
design and synthesis of 4-anilino-5-carboxamido-2-pyridone MEK1 inhibitors using a combination of medicinal chemistry, computational chemistry, and structural elucidation, overview. Binding structure analysis, overview
-
additional information
no inhibition of MEK2 by MEK1/ERK1/2-specific inhibitor PD98059
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
-
MKK3 expression is induced upon Pseudomonas syringae infection
-
additional information
light signals activate the MAP kinase via phosphorylation through MAP kinase kinase
-
additional information
-
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview
-
additional information
-
activation is induced by epidermal growth factor tyrosine protein kinase and nucelar growth factor tyrosine protein kinase
-
additional information
-
enzyme is activated by environmental stress and physiological stimuli. In hematopoietic cells, endogenous MKK7 is activated by treatment with the growth factor interleukin-3, or by ligation of CD40, the B-cell antigen receptor, or the receptor for the Fc fragment of immunoglobulin. MKK7 is also activated when cells are exposed to heat, UV irradiation, anisomycin, hyperosmolarity or the pro-inflammatory cytokine tumor necrosis factor-alpha
-
additional information
-
MEK6 is strongly activated by UV, anisomycin, and osmotic shock
-
additional information
-
the enzyme is activated in cells treated with tumor necrosis factor-alpha
-
additional information
-
MEK, ERK-1 and ERK-2 are activated by phosphorylation by B-Raf, the B-Raf mutant V590E activates the enzymes constitutively and independently of Ras, which leads to melanoma cell proliferation
-
additional information
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview; MKKs are activated by phopshorylation through MKKKs, overview
-
additional information
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview; MKKs are activated by phopshorylation through MKKKs, overview
-
additional information
-
dissociation factor DF induces MEK1/2 and ERK1/2 expression
-
additional information
-
ERK and MEK are activated by phosphorylation, ERK is induced by formalin
-
additional information
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview; MKKs are activated by phopshorylation through MKKKs, overview
-
additional information
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview; MKKs are activated by phopshorylation through MKKKs, overview
-
additional information
-
the enzyme is activated by phosphorylation through a specific mitogen-activated protein kinase kinase kinase
-
additional information
-
activation in vivo in response to serum, phosphorylation and activation by the v-Raf protein in vitro
-
additional information
activated by GTP-Cdc42 or GTP-Rac1 in vitro
-
additional information
-
MEK, ERK-1 and ERK-2 are activated by phosphorylation, tetanus toxin or the C-terminal part of the heavy chain induce phosphorylation of ERK-1 and ERK-2 at Thr202 and Tyr204
-
additional information
-
neurotrophin induces mitogen-activated protein kinase kinase signaling, which is antagonized by semaphorin 3F, Gab-1, an adaptor protein, is recruited by the TrkA kinase to activate MEK in sympathetic neurons, Gab-1 can reverse semaphorin 3F inhibition of the MEK activation
-
additional information
-
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview
-
additional information
-
Pbs2p is activated by MAP kinase kinase kinases Ssk2p and Ssk22p that are under the control of the SLN1-SSK1 two-component osmosensor. Alternatively, Pbs2p is activated by a mechanism that involves the binding of its amino terminal proline-rich motif to the Src homology 3 domain of a putative transmembrane osmosensor Sho1p
-
additional information
-
MKKs are activated by phopshorylation through MKKKs, activation mechanism of MKK4 involving MEKK1, overview
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
additional information
-
Michaelis-Menten kinetics; Michaelis-Menten kinetics
-
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.01
1-(2,3-dihydroxypropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above, cascade IC50
0.00489 - 0.0049
1-(3-cyanopropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000091 - 0.01
1-allyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.001
1-ethyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.003
1-methyl-4-(2-naphthylamino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.0000174
3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
Mus musculus
P31938, Q63932
cascade IC50
0.00254 - 0.005
4-(2-fluoro-4-iodoanilino)-1-(2-hydroxyethyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.003
4-(2-fluoro-4-iodoanilino)-1-(3-hydroxypropyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above, cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000004 - 0.000023
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000425 - 0.005
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylic acid
0.00113
4-(2-fluoro-4-iodoanilino)-1-[2-(2-methoxyethoxy)ethyl]-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00043 - 0.00254
4-(2-fluoro-4-iodoanilino)-6-oxo-1-propyl-1,6-dihydro-3-pyridinecarboxamide
0.000195
4-(2-fluoro-4-iodoanilino)-N,1-dimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000627 - 1.2
4-(2-fluoro-4-iodoanilino)-N,N,1-trimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000005 - 0.000018
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.00018 - 0.00021
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000061 - 0.000095
4-(2-fluoro-4-iodoanilino)-N-(3-hydroxypropyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.00297
4-(2-fluoro-4-methylanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00015 - 0.00036
4-(2-fluoro-4-methylsulfanylphenylamino)-1-methyl-6-oxo-1,6-dihydro-3 -pyridinecarboxamide
0.0039 - 0.00572
4-(3,4-dichlorophenylamino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000093 - 0.00191
4-(4-bromo-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.00012 - 0.00363
4-(4-bromo-2-fluoroanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.0000068 - 0.000124
4-(4-bromo-2-fluorophenylamino)-1-methylpyridin-2(1H)-one
Homo sapiens
-
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 deriva
0.01
4-(4-cyano-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above, cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00011 - 0.00262
4-(4-ethyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.000021 - 0.0001
4-(4-ethynyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
0.0000842
4-amino-1-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl]-2-hydroxybutan-1-one
Mus musculus
P31938, Q63932
cascade IC50
0.01
4-[2-fluoro-4-(1,1,2,2,3,3,4,4,4-nonafluorobutyl)anilino]-1-methyl-6-oxo-1,6 -dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above, cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.01
4-[2-fluoro-4-(3-hydroxypropyl)anilino]-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above, cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.0000012
4-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl]-3-hydroxy-4-oxobutanamide
Mus musculus
P31938, Q63932
cascade IC50
0.000052
AS-703026
Homo sapiens
-
inhibition of MEK1, pH and temperature not specified in the publication
0.0000052
CH4987655
Homo sapiens
-
inhibition of MEK1, pH and temperature not specified in the publication
0.000063 - 0.000669
ethyl 4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylate
0.00067
ethyl 4-(2-fuoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylate
Mus musculus
P31938, Q63932
cascade IC50
-
0.000046
LL-Z1640-2
Homo sapiens
-
inhibition of MEK1, pH and temperature not specified in the publication
0.000014
selumetinib
Homo sapiens
-
inhibition of MEK1 phosphorylation of ERK2, pH and temperature not specified in the publication
0.01
tert-butyl [5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetate
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.01
[5-(aminocarbonyl)-4-(2-fluoro-4-iodoanilino)-2-oxo-1(2H)-pyridinyl]acetic acid
Mus musculus
P31938, Q63932
above, cascade IC50
0.00489
1-(3-cyanopropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.0049
1-(3-cyanopropyl)-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.000091
1-allyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00601
1-allyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.01
1-allyl-4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00254
4-(2-fluoro-4-iodoanilino)-1-(2-hydroxyethyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.005
4-(2-fluoro-4-iodoanilino)-1-(2-hydroxyethyl)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
above cascade IC50; colon26 cellular assay
0.000004
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.000023
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000425
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylic acid
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.005
4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylic acid
Mus musculus
P31938, Q63932
colon26 cellular assay
0.0001
4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00063
4-(2-fluoro-4-iodoanilino)-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.00043
4-(2-fluoro-4-iodoanilino)-6-oxo-1-propyl-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.00254
4-(2-fluoro-4-iodoanilino)-6-oxo-1-propyl-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000627
4-(2-fluoro-4-iodoanilino)-N,N,1-trimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
1.2
4-(2-fluoro-4-iodoanilino)-N,N,1-trimethyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.000005
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.000018
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00018
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.000206
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00021
4-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.000061
4-(2-fluoro-4-iodoanilino)-N-(3-hydroxypropyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000095
4-(2-fluoro-4-iodoanilino)-N-(3-hydroxypropyl)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assayy
0.00015
4-(2-fluoro-4-methylsulfanylphenylamino)-1-methyl-6-oxo-1,6-dihydro-3 -pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.000356
4-(2-fluoro-4-methylsulfanylphenylamino)-1-methyl-6-oxo-1,6-dihydro-3 -pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00036
4-(2-fluoro-4-methylsulfanylphenylamino)-1-methyl-6-oxo-1,6-dihydro-3 -pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.0039
4-(3,4-dichlorophenylamino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.0057
4-(3,4-dichlorophenylamino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.00572
4-(3,4-dichlorophenylamino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000093
4-(4-bromo-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.0019
4-(4-bromo-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50
0.00191
4-(4-bromo-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00012
4-(4-bromo-2-fluoroanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.00363
4-(4-bromo-2-fluoroanilino)-N-(2-hydroxyethoxy)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.00011
4-(4-ethyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.00262
4-(4-ethyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000021
4-(4-ethynyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
colon26 cellular assay
0.0001
4-(4-ethynyl-2-fluoroanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxamide
Mus musculus
P31938, Q63932
cascade IC50; inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000019
BAY 869766
Homo sapiens
-
inhibition of MEK1, pH and temperature not specified in the publication
0.000047
BAY 869766
Homo sapiens
-
inhibition of MEK2, pH and temperature not specified in the publication
0.000016
CI-1040
Mus musculus
P31938, Q63932
clinical candidate, inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
0.000063
ethyl 4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylate
Mus musculus
P31938, Q63932
colon26 cellular assay
0.000669
ethyl 4-(2-fluoro-4-iodoanilino)-1-methyl-6-oxo-1,6-dihydro-3-pyridinecarboxylate
Mus musculus
P31938, Q63932
inhibition of the Raf-MEK-ERK cascade in an isolated enzyme assay
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
large scale activity assay with recombinant enzyme in a protein chip consisting of a microwell array with protein covalently attached to the wells via a 3-glycidoxypropyltrimethoxysilane crosslinker, overview
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.2
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
30
37
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pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
isolated from a smoke tree, Cotinuscoggygria in Fragrant Hills Park,Beijing
-
-
brenda
isolated from a smoke tree, Cotinuscoggygria in Fragrant Hills Park,Beijing
-
-
brenda