Information on EC 2.7.10.2 - non-specific protein-tyrosine kinase and Organism(s) Homo sapiens and UniProt Accession O60674

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UNIPROT: O60674
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The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.10.2
-
RECOMMENDED NAME
GeneOntology No.
non-specific protein-tyrosine kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
SYSTEMATIC NAME
IUBMB Comments
ATP:[protein]-L-tyrosine O-phosphotransferase (non-specific)
Unlike EC 2.7.10.1, receptor protein-tyrosine kinase, this protein-tyrosine kinase does not have a transmembrane domain. In the human genome, 32 non-specific protein-tyrosine kinases have been identified and these can be divided into ten families [1].
CAS REGISTRY NUMBER
COMMENTARY hide
114051-78-4
p56lck protein kinase
80449-02-1
protein-tyrosine kinase
9026-43-1
this CAS Reg. No. encompasses a great variety of protein kinases including the serine/threonine specific kinases
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
constitutive JAK activation leads to persistent activation of STAT transcription factors, and several cancers exhibit constitutive STAT activation, in the absence of JAK or STAT activating mutations
malfunction
physiological function
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]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [peptide]-L-tyrosine
ADP + a [peptide]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + a [Tyr-2 peptide]-L-tyrosine
ADP + a [Tyr-2 peptide]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + A-kinase anchor protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
ATP + arsenate resistance protein ARS2
?
show the reaction diagram
-
-
-
-
?
ATP + ataxin 2 related protein
?
show the reaction diagram
-
-
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + Bcl-2-associated transcription factor 1
?
show the reaction diagram
-
-
-
-
?
ATP + beta 1-integrin cytoplasmic domain peptide
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + biotin-GGEAIYAAPFKK-amide
ADP + phosphorylated biotin-GGEAIYAAPFKK-amide
show the reaction diagram
-
a peptide with the preferred c-Abl substrate sequence carrying an Nterminal biotin
-
-
?
ATP + c-Src
?
show the reaction diagram
-
-
-
-
?
ATP + calponin 3
?
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + cdc2(6-20) peptide
?
show the reaction diagram
-
i.e. KVEKIGEGTYGVVYK, substrate of Src family kinases
-
-
?
ATP + chromosome 20 open reading frame 77
?
show the reaction diagram
-
-
-
-
?
ATP + cleavage and polyadenylation specific factor 5
?
show the reaction diagram
-
-
-
-
?
ATP + cofilin
ADP + phosphorylated cofilin
show the reaction diagram
phosphorylation specifically at Ser-3
-
-
?
ATP + cortactin
?
show the reaction diagram
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
ATP + EEEEY
ADP + EEEE(phospho)Y
show the reaction diagram
-
-
-
-
?
ATP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G
ADP + EEEEYIQ[dP]-8-hydroxy-5-(N,N-dimethylsulfonamido)-2-methylquinoline-G phosphate
show the reaction diagram
-
Y7 Sox-based substrate, kinetic assay
-
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
ATP + EQEDEPEGDYFEWLE
ADP + EQEDEPEGDpYFEWLE
show the reaction diagram
-
-
-
-
?
ATP + eukaryotic translation initiation factor 3, subunit 4
?
show the reaction diagram
-
-
-
-
?
ATP + ewing sarcoma breakpoint region 1
?
show the reaction diagram
-
-
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + F peptide
ADP + phospho-L-tyrosinyl-F peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIFGEI-NH2
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + FUS interacting protein (serine/arginine rich) 1
?
show the reaction diagram
-
-
-
-
?
ATP + FUS/TLS oncogene
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + FUSE binding protein 2
?
show the reaction diagram
-
-
-
-
?
ATP + GAPEVIYATPGAKKK
ADP + GAPEVI-phosphotyrosinyl-ATPGAKKK
show the reaction diagram
-
consensus substrate
-
-
?
ATP + GGEAIYAAPFKK
ADP + GGEAIYAAPFKK phosphate
show the reaction diagram
-
kinase assay using biotinylated model substrate peptide
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein A3
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein AB
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein D-like
?
show the reaction diagram
-
-
-
-
?
ATP + heterogeneous nuclear ribonucleoprotein K
?
show the reaction diagram
-
-
-
-
?
ATP + histone
ADP + phosphorylated histone
show the reaction diagram
serine/threonine-specific kinase activity
-
-
?
ATP + homeobox prox 1
?
show the reaction diagram
-
-
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
ATP + KVEKIGEGTYGVVYK
ADP + ?
show the reaction diagram
-
synthetic peptide substrate
-
-
?
ATP + lysozyme-L-tyrosine
ADP + lysozyme-L-tyrosine phosphate
show the reaction diagram
-
substrate of Src, low activity with Csk or Chk
-
-
?
ATP + myelin basic protein
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + NEFA-interacting nuclear protein
?
show the reaction diagram
-
-
-
-
?
ATP + NICE-4
?
show the reaction diagram
-
-
-
-
?
ATP + P1 peptide
ADP + phospho-L-tyrosinyl-P1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIpYGEI-NH2
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu,Tyr)
? + ADP
show the reaction diagram
-
substrate used in the tyrosine kinase asssay
-
-
?
ATP + poly(Glu-Tyr)
? + ADP
show the reaction diagram
-
substrate used in the activity assay
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu-Tyr)-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + poly(Glu4-Tyr)
ADP + poly(Glu4-Tyr)-L-tyrosine phosphate
show the reaction diagram
ATP + proteasome activator subunit 3
?
show the reaction diagram
-
-
-
-
?
ATP + protein
?
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + RasGAP SH3-domain binding protein
?
show the reaction diagram
-
-
-
-
?
ATP + recombinant GST/beta3 integrin cytoplasmic tail peptide
ADP + ?
show the reaction diagram
-
-
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 10
?
show the reaction diagram
-
-
-
-
?
ATP + RNA binding motif protein 4B
?
show the reaction diagram
-
-
-
-
?
ATP + S1 peptide
ADP + phospho-L-tyrosinyl-S1 peptide
show the reaction diagram
-
i.e. biotin-Aca-AAAEEIYGEI-NH2
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + signal transducer and activator of transcription
ADP + phospho-L-tyrosinyl-signal transducer and activator of transcription
show the reaction diagram
-
-
-
-
?
ATP + similar to zinc finger CCCH-type domain-containing protein 6
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor proline/glutamine-rich
?
show the reaction diagram
-
-
-
-
?
ATP + splicing factor, arginine/serine-rich9
?
show the reaction diagram
-
-
-
-
?
ATP + Src
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
wild-type Src and catalytically inactive mutant Src K295M, terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site, Glu510 of Src interacts with Arg283 of Csk in Csk-Src recognition, activity with Src fragments, overview
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-L-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
ATP + thyroid hormone receptor associated protein 3
?
show the reaction diagram
-
-
-
-
?
ATP + TRK-fused gene
?
show the reaction diagram
-
-
-
-
?
ATP + Tyr267 of Vav1
ADP + phosphorylated Tyr267 of Vav1
show the reaction diagram
-
-
isoform c-Abl kinase probably regulates the activity of Rho guanine exchange factor Vav1 by direct phosphorylation at Tyr267 in the Dbl homology domain. The C-terminal SH3-SH2-SH3 domain and proline-rich region of Vav1 are required for its interaction with c-Abl kinase
-
?
ATP + zinc finger, CCHC domain containing protein 8
?
show the reaction diagram
-
-
-
-
?
ATP + [Abi1]-L-tyrosine
ADP + [Abi1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl phosphorylates Y213 of Abi1
-
-
?
ATP + [actin-stabilizing adapter protein HS1]-L-tyrosine
ADP + [actin-stabilizing adapter protein HS1]-L-tyrosine phosphate
show the reaction diagram
-
c-Abl binds to phospho-HS1 via its SH2 domains and is required for full tyrosine phosphorylation of HS1 during T-cell activation
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
ATP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine
ADP + [carrier protein-intein-CAEEEIYGEFEA]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CAEEEIYGEFEA derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGKYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGKYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTFGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTFGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTpYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTpYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYFVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYFVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVEYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVEYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVFK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVFK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGEGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGEGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine
ADP + [carrier protein-intein-CIGKGTYGVVYK]-L-tyrosine phosphate
show the reaction diagram
-
substrate is synthesized by fusing a 27 kDa carrier protein to intein which is linked to the peptide CIGKGTYGVVYK derived from human cyclin-dependent kinase harboring a phosphorylation site for Src kinase
-
-
?
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion, estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen receptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
ATP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine
ADP + [hyperpolarization-activated, cyclic nucleotide-gated 4 channel]-L-tyrosine phosphate
show the reaction diagram
-
substrate HCN4, tyrosine 531 is phosphorylated
-
-
?
ATP + [kdSrc kinase]-L-tyrosine
ADP + [kdSrc kinase]-L-tyrosine phosphate
show the reaction diagram
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + [Sam68]-L-tyrosine
ADP + [Sam68]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [tubulin]-L-tyrosine
ADP + [tubulin]-L-tyrosine phosphate
show the reaction diagram
-
highly active with c-Fes, which also catalyzes tubulin polymerization in vitro
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
ATP + [[Lys19]Cdc2-(6-20) peptide]-L-tyrosine
?
show the reaction diagram
-
i.e. KVEKIGEGTYGVVKK
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
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]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + a [homeodomain-interacting protein kinase 2]-L-tyrosine
ADP + a [homeodomain-interacting protein kinase 2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + a [protein]-L-tyrosine
ADP + a [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + Abl
ADP + phospho-L-tyrosinyl-Abl
show the reaction diagram
-
Abl is an important substrate for Src signalling in normal cells
-
-
?
ATP + Bad protein
ADP + phosphotyrosinyl Bad protein
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + beta-catenin
ADP + phospho-tyrosinyl-beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + Cas protein
ADP + phospho-tyrosinyl-Cas protein
show the reaction diagram
-
-
-
-
?
ATP + cortactin
ADP + phospho-tyrosinyl-cortactin
show the reaction diagram
-
-
-
-
?
ATP + cyclin-associated cyclin-dependent kinase
ADP + phosphorylated cyclin-associated cyclin-dependent kinase
show the reaction diagram
P30291
Wee1 negatively regulates cyclin-dependent kinases by phosphorylation on Y15
-
?
ATP + epidermal growth factor receptor
ADP + phospho-L-tyrosinyl-epidermal growth factor receptor
show the reaction diagram
-
the activated Abl tyrosine kinase negaively regulates endocytosis of the epidermal growth factor, e.g. in NR6 cells, overview, Abl allows the ligand-activated EGFR to escape Cbl-dependent down-regulation by inhibiting the accumulation of Cbl at the plasma membrane in response to epidermal growth factor stimulation and disrupting the formation of the EGFR-Cbl complex without affecting Cbl protein stability
-
-
?
ATP + ezrin
ADP + phospho-tyrosinyl-ezrin
show the reaction diagram
-
-
-
-
?
ATP + FAK
ADP + phospho-tyrosinyl-FAK
show the reaction diagram
-
-
-
-
?
ATP + glycogen synthase kinase 3beta
ADP + phosphotyrosinyl glycogen synthase kinase 3beta
show the reaction diagram
-
substrate of Akt
-
-
?
ATP + IkappaBalpha-L-tyrosine
ADP + IkappaBalpha-L-tyrosine phosphate
show the reaction diagram
-
p56lck regulates cell motility and nuclear factor kappaB-mediated secretion of urokinase type plasminogen activator through tyrosine phosphorylation of IkappaBalpha following hypoxia/reoxygenation, molecular mechanism, physiological role
-
-
?
ATP + NaV1.2 channel
ADP + phospho-L-tyrosinyl-NaV1.2 channel
show the reaction diagram
-
Y66 and Y1893, which are in consensus sequences appropriate for binding to the Fyn SH2 domain after phosphorylation, are both required for optimal binding and regulation by Fyn. Y730, which is located near the SH3-binding motif in LI-II, and Y1497 and Y1498 in the inactivation gate in LIII-IV, are also required for optimal regulation, but phosphorylation of these sites likely promotes fast inactivation
-
-
?
ATP + p120 protein
ADP + phospho-tyrosinyl-p120 protein
show the reaction diagram
-
-
-
-
?
ATP + p190 GTPase
ADP + phospho-tyrosinyl-p190 GTPase
show the reaction diagram
-
-
-
-
?
ATP + p34cdc2
ADP + phosphorylated p34cdc2
show the reaction diagram
-
Wee1 kinase inhibits mitosis by directly phosphorylating p34cdc2 on Y15
-
?
ATP + PAK1
ADP + phospho-L-tyrosinyl-PAK1
show the reaction diagram
-
Jak2 is involved in the regulation of serine-threonine kinase PAK1, maximal cell motility is required for tyrosyl phosphorylation of PAK1
-
-
?
ATP + paxillin
ADP + phospho-tyrosinyl-Shc paxillin
show the reaction diagram
-
-
-
-
?
ATP + PIKE-A
ADP + phosphotyrosinyl-PIKE-A
show the reaction diagram
-
i.e. phosphatidylinositol 3-kinase enhancer-activating Akt, phosphorylation by fyn is essential for PIKE-A complex formation and apoptotic cleavage, overview
-
-
?
ATP + plakoglobin
ADP + phospho-tyrosinyl-plakoglobin
show the reaction diagram
-
-
-
-
?
ATP + protein
?
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus. By regulating the activity of these kinases, CSK may play an important role in cell growth and development
-
-
?
ATP + protein
ADP + protein tyrosine phosphate
show the reaction diagram
-
CSK phosphorylates other members of the src-family of tyrosine kinases at their regulatory carboxy-terminus
-
-
?
ATP + protein tyrosine
ADP + protein tyrosine phosphate
show the reaction diagram
-
p135tyk2 tyrosine kinase directly binds and tyrosine phosphorylates alpha subunit of the type I IFN receptor, IFN-R
-
-
?
ATP + protein tyrosine kinase Yes
ADP + phospho-L-tyrosinyl Yes
show the reaction diagram
-
Csk inactivates the enzyme substrate
-
-
?
ATP + Rho protein
ADP + phospho-tyrosinyl-Rho protein
show the reaction diagram
-
-
-
-
?
ATP + Shc protein
ADP + phospho-tyrosinyl-Shc protein
show the reaction diagram
-
-
-
-
?
ATP + Src family kinase
?
show the reaction diagram
-
substrate of the protein kinases CSK and CHK, which specifically phosphorylate a tyrosine residue at the C-terminus forming intramolecular bonds to the SH2 domain and inhibiting the Src family kinase, overview
-
-
?
ATP + Src family kinase
ADP + phospho-L-tyrosinyl Src family kinase
show the reaction diagram
-
terminal Src kinase Csk specifically phosphorylates Src family kinases on a C-terminal Tyr residue, which down-regulates their activities, identification of the docking determinants in Src recognized by the Csk substrate-docking site
-
-
?
ATP + Src protein
ADP + Src protein phosphate
show the reaction diagram
P42679
MATK can phosphorylate the carboxyl-terminal conserved tyrosine of the Src protein
-
-
?
ATP + STAT3
ADP + phospho-tyrosinyl-STAT3
show the reaction diagram
-
-
-
-
?
ATP + Tc10/Cdc42 GTPase-activating protein
ADP + phospho-L-tyrosinyl-Tc10/Cdc42 GTPase-activating protein
show the reaction diagram
-
physical and functional interaction of Fyn with the brain-enriched Rho GTPase-activating protein Tc10/Cdc42 GTPase-activating protein, i.e. TCGAP, TCGAP is involved in Fyn-mediated regulation of axon and dendrite outgrowth
-
-
?
ATP + [androgen receptor]-L-tyrosine
ADP + [androgen receptor]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [aryl hydrocarbon receptor]-L-tyrosine
ADP + [aryl hydrocarbon receptor]-L-tyrosine phosphate
show the reaction diagram
-
Src tyrosine kinases are involved in a signaling transduction pathway activating aryl hydrocarbon receptor AhR-mediated signalling by omeprazole or 2,3,7,8-tetrachlorodibenzo-4-dioxin TCDD ligand-binding, AhR phosphorylation at Tyr320, the omeprazole-dependent mechanism probably involves S318 and K316
-
-
?
ATP + [c-Cbl]-L-tyrosine
ADP + [c-Cbl]-L-tyrosine phosphate
show the reaction diagram
-
proto-oncogenic PTK protein substrate
-
-
?
ATP + [estrogen receptor alpha]-L-tyrosine
ADP + [estrogen receptor alpha]-L-tyrosine phosphate
show the reaction diagram
-
-
estrogen receptor alpha associates with c-Abl nonreceptor tyrosine kinase. The direct interaction is mediated by two PXXP motifs of estrogen receptor alpha and the c-Abl SH3 domain. Estrogen receptor alpha can be phosphorylated on residues Y52 and Y219. Phosphorylation by c-Abl stabilizes estrogen recptor alpha, resulting in enhanced estrogen receptor alpha transcriptional activity and increased expression of endogenous target genes. Phosphorylation at the Y219 site affects DNA binding and dimerization by estrogen receptor alpha. c-Abl kinase activity is required for regulation of the estrogen receptor alpha function, and a Y52F/Y219F mutant estrogen receptor leads to reduced breast cancer cell growth and invasion
-
?
ATP + [fibroblast growth factor receptor FGFR2]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR2]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [fibroblast growth factor receptor FGFR3]-L-tyrosine
ADP + [fibroblast growth factor receptor FGFR3]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2, interaction via the FGFR juxtamembrane and the Pyk2 kinase domain, activation is antagonized by tyrosine phosphatase Shp2
-
-
?
ATP + [P-110]-L-tyrosine
ADP + [P-110]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine
ADP + [p110 catalytic subunit of PI 3-kinase]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p21Cip1]-L-tyrosine
ADP + [p21Cip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p27Kip1]-L-tyrosine
ADP + [p27Kip1]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [p57Kip2]-L-tyrosine
ADP + [p57Kip2]-L-tyrosine phosphate
show the reaction diagram
-
-
-
-
?
ATP + [parkin]-Tyr143
ADP + [parkin]-phospho-Tyr143
show the reaction diagram
-
-
nonreceptor tyrosine kinase c-Abl phosphorylates tyrosine 143 of parkin, which encodes a ubiquitin E3 ligase, related to autosomal recessive Parkinson disease. Phosphorylation inhibits parkin's ubiquitin E3 ligase activity and protective function
-
?
ATP + [protein]-L-tyrosine
ADP + [protein]-L-tyrosine phosphate
show the reaction diagram
ATP + [Src-family protein tyrosine kinase]-L-tyrosine
ADP + [Src-family protein tyrosine kinase]-L-tyrosine phosphate
show the reaction diagram
-
i.e. SFK, substrate of protein tyrosine kinases Csk and Chk, phosphorylation at the regulatory tyrosine leading to inhibition of the SFK
-
-
?
ATP + [Stat5B]-L-tyrosine
ADP + [Stat5B]-L-tyrosine phosphate
show the reaction diagram
-
activation by non-receptor tyrosine kinase Pyk2
-
-
?
ATP + [transmembrane adaptor protein LAT]-L-tyrosine
ADP + [transmembrane adaptor protein LAT]-L-tyrosine phosphate
show the reaction diagram
-
substrate of ZAP-70
-
-
?
ATP + [ZAP-70]-L-tyrosine
ADP + [ZAP-70]-L-tyrosine phosphate
show the reaction diagram
-
substrate of Lck, Fyn, and c-Abl, leads to ZAP-70 activation, mechanism
-
-
?
gelsolin + ATP
phospho-tyrosinyl gelsolin + ADP
show the reaction diagram
-
phosphorylation by PYK2 increases the binding of gelsolin to phosphoatidylinositol lipids and actin polymerization at the fibroblastic cell periphery
-
-
?
p130Cas + ATP
phospho-tyrosinyl p130Cas + ADP
show the reaction diagram
-
phosphorylation of the Crk and Nck adaptor protein by Fak
-
-
?
paxillin + ATP
phospho-tyrosinyl paxillin + ADP
show the reaction diagram
-
phosphorylation at Tyr31 and Tyr118 by Fak plays a role in tumor cell motility inhibition
-
-
?
STAT transcription activator protein + ATP
phosphorylated STAT transcription activator protein + ADP
show the reaction diagram
-
activation of STAT by phosphorylation is required for translocation to the nucleus, the enzyme regulates the cytokine expression via STAT, overview
-
-
?
Wiskott-Aldrich syndrome protein + ATP
phospho-tyrosinyl Wiskott-Aldrich syndrome protein + ADP
show the reaction diagram
-
i.e. WASP, phosphorylation by Fak
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Fe3+
-
when Lyn or Hck kinases, which have been stabilised in the inactive state by phosphorylation of the C-terminal regulatory tyrosine, are incubated with Fe3+ ions, a significant enhancement of kinase activity is observed
Zn2+
-
-
additional information
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
AZ960
-
potent and selective ATP competitive inhibitor of JAK2 enzyme activity
INCB018424
-
Jak2 inhibitor
JAK-inhibitor I
-
40% JAK2 residual activity in the presence of 0.002 mM JAK-inhibitor I and 0.02 mM ATP
-
LS104
-
i.e. [(E,E)-2-(benzylaminocarbonyl)-3-(3,4-dihydroxystyryl)acrylonitrite], non-ATP-competitive small-molecule inhibitor of JAK2, 20% residual activity of mutant V617F in the resence of 0.02 mM LS104 and 0.02 mM ATP
TG101209
-
Jak2 inhibitor
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
-
(2E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide
-
WP1066
(2E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
-
LS104
(2E,4E)-N-benzyl-2-cyano-5-(3,4-dihydroxyphenyl)penta-2,4-dienamide
-
AG490, potent JAK2 inhibitor
1-azaanthraquinones
-
-
-
1-methyl-emodin
-
inhibition of p56lck and c-Src
-
2,5-dihydroxy-3-(3,4-dihydroxyphenyl)-6-phenyl-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,5-dihydroxy-3-phenyl-6-(3,4,5-trihydroxyphenyl)-1,4-benzoquinone
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2,7,8-trihydroxy-3-phenyl-1,4-dibenzofurandione
-
secondary metabolite isolated from fungus Stilbella sp. strain 1586
2-(1,1-dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one
-
i.e. JAK inhibitor-I
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
-
2-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
2-chloro-omega-hydroxy-emodin
-
inhibition of p56lck and c-Src
-
2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
-
2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-one
-
potent pan-JAK inhibitor
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
-
3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
-
-
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
-
3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
-
CP-690,550 JAK3-specific inhibitor
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
-
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
-
4-amino-5-(4-chlorophenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine
-
PP2, AG-1897
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
4-amino-5-(4-chlorophenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d] pyrimidine
-
4-amino-5-(4-methylphenyl)-7-(tert-butyl)pyrazolo[3,4-d]pyrimidine
-
i.e. pp1, inhibits Src family members like Lyn, no inhibition of Syk
-
4-chloro-N-[5-[(3-chlorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-chloro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(3-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-fluorobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-methoxybenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-fluoro-N-[5-[(4-nitrobenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
4-methyl-3-[[3-(pyrimidin-4-yl)pyridin-2-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide
-
-
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
-
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
-
inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo
8-methyl-emodin
-
inhibition of p56lck and c-Src
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
-
-
9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
-
-
9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
-
9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
-
9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
-
A-419259
-
-
-
acacetin
-
inhibition of p56lck
AcpYEEI
-
ATP-phosphopeptide conjugate
ADP
-
competitive versus ATP, noncompetitive versus S1 peptide
AG-490
-
inhibits JAK2 tyrosine kinase
AG1024
-
-
AG490
alsterpaullone
-
at 0.01 mM: 66% inhibition of CHK, 81% inhibition of LCK, and 10% inhibition of CSK
AMN107
-
a specific BCR-ABL tyrosine kinase inhibitor, Abl binding structure, in vivo inhibition study in chronic myeloid leukemia, CML, overview
AP23464
apigenin
-
inhibition of p56lck
AST-487
-
-
-
ATP-1,13-Trioxa-SA-phospho-Tyr-g-p-azido-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-1,13-Trioxa-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-1,8-Diam-Suc-1,8-Diam-Suc-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-11-Aund-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-6-Ahex-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-8-Aoct-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-beta-Ala-phospho-Tyr-Glu-Glu-Ile-OH
-
inhibition of SH2 domain tyrosine protein kinases
-
ATP-gamma-S
-
-
AZD-1480
-
Jak2 inhibitor
AZD0530
-
-
AZM 475271
-
-
BAY61-3606
-
-
Bcr protein
-
negative regulator
-
bengamide A
-
c-Src from bengamide A-treated cells retains its N-terminal methionine and suffers a decrease in N-terminal myristoylation, which is accompanied by a shift of its subcellular distribution from the plasma membrane to the cytosol, and decreased tyrosine kinase activities of c-Src both in vitro and in vivo and eventually delayed cell-cycle progression through G2/M, overview, bengamide A reduced tyrosine phosphorylation on a few proteins, and is not a general tyrosine kinase inhibitor
bisindolylmaleimide I
-
blocks alboaggregin-A activation of Fyn
bosutinib
C-terminal Src kinase
-
i.e. CSK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
catenarin
-
i.e. 4-hydroxy-emodin, inhibition of p56lck and c-Src
caveolin
-
a non-catalytic inhibitor of SFKs, transient inhibition
-
CGP 76030
-
-
CGP 77675
-
-
CGP76030
-
growth-inhibitory in vivo
Chk
-
i.e. Csk-homologous kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, Chk is also a 'non-catalytic inhibitor' binding directly to the SFK forming stable complexes and inhibiting it, mechanism, overview
-
chrysin
-
inhibition of p56lck
CMP6
-
i.e. 2-tert-butyl-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinoline-7-1, specific for JAK2, kinase domain binding structure and mechanism
-
CP-690 550
-
Jak3 and Jak2 inhibitor
CP-690,550
CP690,550
-
targeting Jak3
Csk
-
i.e. C-terminal Src kinase, a catalytic inhibitor of SFKs phosphorylating the regulatory tyrosine residue of SFK which leads to inhibition of SFK, mechanism, overview
-
CSK-homologous kinase
-
i.e. CHK, an inhibitor which inactivates Src family of protein kinases by phosphorylating a consensus tyrosine YT near the C terminus, phosphorylated YT then intramolecularly binds to the enzyme's SH2 domain, pYT/SH2 interaction, together with binding between the SH2 kinase linker and the SH3 domain, stabilizes the enzyme in a closed inactive conformation, a second non-catalytic inhibitory mechanism involves tight binding of CHK to the enzyme's SFKs. The binding alone is sufficient to inhibit SFKs inhibition, preparation of recombinant SH2 and SH3 domains by expression in Escherichia coli, overview
-
curcumin
damnacanthal
-
an anthraquinone, strong and selective inhibition of p56lck
dasatinib
datiscetin
-
inhibition of p56lck
emodic acid
-
inhibition of p56lck and c-Src
emodin
emodin derivatives
-
synthetic analogues, inhibition of p56lck and Src, overview
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endocrocin
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inhibition of p56lck and c-Src
epihematoxylol
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F-actin
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negative regulator
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Fe3+
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Lyn or Hck kinases in the unphosphorylated active state are significantly inhibited by Fe3+ ion
fisetin
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inhibition of p56lck
flavone derivatives
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inhibition of p56lck, overview
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Fus1 protein
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negative regulator
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galangin
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inhibition of p56lck
genistein
genkwanin
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inhibition of p56lck
Gleevec
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also known as STI-571 or imatinib
haematoxylene
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haematoxylone
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hematoxylin
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Hg2+
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at PO2 of about 20 mM
iclusig
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potent inhibitor of Abl
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imatinib
imatinib mesylate
INCB018424
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Jak2 inhibitor
INCB16562
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selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3
INCB18424
INCB20
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potently inhibits all members of the JAK family with a 100-1000fold selectivity for JAKs over more than 70 other kinases, potent and specific Pan-JAK inhibitor
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indirubin-3'-monoxime
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at 0.01 mM: 62% inhibition of CHK, 89% inhibition of LCK, but no inhibition of CSK
INNO-406
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previously NS-187, inhibits ABL1
interdomain B
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connects the enzyme's catalytic kinase domain with its SH2 domain, is responsible for regulatory autoinhibition of ZAP-70 involving Tyr315 and Tyr319, deletion of the interdomain B preserves enzyme function, the regulation mechanism is similar to receptor protein tyrosine kinase EphB2, EC 2.7.10.1, overview
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ITF2357
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Jak2 inhibitor
kaempferide
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inhibition of p56lck
kaempferol
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inhibition of p56lck
kaempferol-3-O-arabinoside
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slight inhibition of p56lck
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kaempferol-3-O-rhamnoside
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slight inhibition of p56lck
kenpaullone
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at 0.01 mM: 35% inhibition of CHK, 85% inhibition of LCK, and 14% inhibition of CSK
lestaurtinib
LFM-A13
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significantly impairs CXCL12-induced human B lymphoma cell line, and blocks Akt activation, homing of transferred B cells to peripheral lymph nodes is impaired, LFM-A13 significantly reduces the CXCL12-induced increases in Ca2+, overview
LS104
luteolin
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inhibition of p56lck
M 475271
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methyl 2,5-dihydroxycinnamate
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i.e. DHC, inhibition of Syk and Lyn
MK-0457
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Jak2 inhibitor
Mn2+
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inhibitory above 1 mM
morin
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inhibition of p56lck
myricetin
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inhibition of p56lck
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
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N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
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N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
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N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine