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Information on EC 3.1.3.48 - protein-tyrosine-phosphatase and Organism(s) Homo sapiens and UniProt Accession Q9UMZ3

for references in articles please use BRENDA:EC3.1.3.48

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IUBMB Comments

Dephosphorylates O-phosphotyrosine groups in phosphoproteins, such as the products of EC 2.7.10.2, non-specific protein-tyrosine kinase.

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms

Synonyms
ptp1b, protein tyrosine phosphatase, shp-1, shp-2, tyrosine phosphatase, protein phosphatase 2a, acid phosphatase activity, mkp-1, cdc25a, ptpn22, more

SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
protein tyrosine phosphatase
-
70Z-SHP
-
-
-
-
alpha-PTP-PEST
-
-
Brain-derived phosphatase
-
-
-
-
BVP
-
-
-
-
CD148
-
-
CD148 antigen
-
-
-
-
CD45 antigen
-
-
-
-
CD45 protein tyrosine phosphatase
-
-
Cdc25 phosphatase
-
-
Cdc25-like protein
-
-
-
-
Cdc25A
Cdc25B
Cdc25B phosphatase
Cdc25C
CDK2-associated dual specificity phosphatase
-
-
-
-
Ch-1PTPase
CPTP1
-
-
-
-
cysteine-dependent protein tyrosine phosphatase
-
-
DEP-1
DLAR
-
-
-
-
DSP18
-
-
dual specificity phosphatase
Dual specificity phosphatase Cdc25A
-
-
-
-
Dual specificity phosphatase Cdc25B
-
-
-
-
Dual specificity phosphatase Cdc25C
-
-
-
-
dual specificity protein phosphatase
-
dual specificity protein phosphatase 23
UniProt
dual specificity protein phosphatase 3
UniProt
Dual specificity protein phosphatase hVH1
-
-
-
-
Dual specificity protein phosphatase hVH2
-
-
-
-
Dual specificity protein phosphatase hVH3
-
-
-
-
Dual specificity protein phosphatase PYST1
-
-
-
-
Dual specificity protein phosphatase PYST2
-
-
-
-
Dual specificity protein phosphatase VHR
-
-
-
-
dual-specificity (Thr/Tyr) MAPK protein phosphatase
-
-
dual-specificity phosphatase
-
dual-specificity phosphatase 5
-
dual-specificity protein tyrosine phosphatase 18
-
-
Dual-specificity tyrosine phosphatase TS-DSP6
-
-
-
-
Dual-specificity tyrosine phosphatase YVH1
-
-
-
-
ES cell phosphatase
-
-
-
-
FAP-1
-
-
HCP
-
-
-
-
HD-PTP
Hematopoietic cell protein-tyrosine phosphatase
-
-
-
-
Hematopoietic cell protein-tyrosine phosphatase 70Z-PEP
-
-
-
-
Hematopoietic protein-tyrosine phosphatase
-
-
-
-
hematopoietic tyrosine phosphatase
-
HEPTP
His domain protein tyrosine phosphatase
-
histidine domain-protein tyrosine phosphatase
-
-
HPTP beta-like tyrosine phosphatase
-
-
-
-
HPTP eta
-
-
-
-
HPTPbeta
-
-
HPTPbeta-CD
-
hPTPE1
-
-
-
-
ICAAR
-
-
-
-
insulinoma associated protein tyrosine phosphatase 2
-
islet cell antigen-related PTP
-
-
Islet cell autoantigen related protein
-
-
-
-
kinase associated phosphatase
-
-
-
-
kinase interaction motif phosphatase
-
L-CA
-
-
-
-
Late protein H1
-
-
-
-
LCA
-
-
-
-
LCA-related phosphatase
-
-
-
-
LDP-3
UniProt
leucocyte common antigen-related protein tyrosine phosphatase
-
-
Leukocyte antigen related
-
-
-
-
leukocyte common antigen-related
-
-
LMW-PTP
low molecular mass dual specificity phosphatase 3
UniProt
Low molecular weight cytosolic acid phosphatase
-
-
-
-
low molecular weight protein tyrosine phosphatase
-
low molecular weight-PTP
-
-
low-molecular-weight protein tyrosine phosphatase
-
-
LRP
-
-
-
-
Lymphoid phosphatase
-
-
-
-
lymphoid-specific tyrosine phosphatase
-
-
M1851
-
-
-
-
MAP kinase phosphatase
-
MAP-kinase phosphatase CPG21
-
-
-
-
MAPK-specific tyrosine phosphatase
-
MEG
-
-
-
-
mitogen-activated protein kinase phosphatase
-
mitogen-activated protein kinase phosphatase-1
-
-
mitogen-activated protein kinase-specific tyrosine phosphatase
-
Mitosis initiation protein
-
-
-
-
Mitosis initiation protein MIH1
-
-
-
-
Mitotic inducer homolog
-
-
-
-
MKP-1
-
trivial names CL100, erp, 3CH134, hVH1
MKP-1 like protein tyrosine phosphatase
-
-
-
-
MKP-2
-
trivial names Typ1, Sty8, hVH2
MKP-3
MKP-4
MKP-5
MKP-7
-
-
MKP-X
-
trivial names Pyst2, B59
MKP1
-
a dual-specificity phosphatase
MKP5-C
catalytic domain of MKP5
MPTP
-
-
-
-
MPTP-PEST
-
-
-
-
NC-PTPCOM1
Neural-specific protein-tyrosine phosphatase
-
-
-
-
non-receptor protein tyrosine phosphatase
-
-
non-receptor tyrosine phosphatase
-
ORF5
-
-
-
-
OST-PTP
osteoclastic protein-tyrosine phosphatase
-
P19-PTP
-
-
-
-
p52shc
-
-
p66shc
-
-
P80
-
-
-
-
PC12-PTP1
-
-
-
-
PCPTP1
UniProt
PEST
-
-
Phogrin
-
-
-
-
Phosphacan
-
-
-
-
phosphatase of regenerating liver-3
-
-
phosphatase, phosphoprotein (phosphotyrosine)
-
-
-
-
phosphatase, phosphotyrosine
-
-
-
-
phosphoprotein phosphatase (phosphotyrosine)
-
-
-
-
phosphotyrosine histone phosphatase
-
-
-
-
phosphotyrosine phosphatase
-
-
-
-
Phosphotyrosine phosphatase 13
-
-
-
-
phosphotyrosine phosphatase 1B
-
-
phosphotyrosine protein phosphatase
-
-
-
-
phosphotyrosine-specific PP
-
-
phosphotyrosylprotein phosphatase
-
-
-
-
PP2A
-
-
Protein phosphatase 1B
-
protein phosphatase 2A
-
-
protein phosphotyrosine phosphatase
-
-
-
-
protein tyrosine phosphatase
protein tyrosine phosphatase 1B
protein tyrosine phosphatase beta
-
protein tyrosine phosphatase epsilon
-
protein tyrosine phosphatase N12
-
protein tyrosine phosphatase N3
-
protein tyrosine phosphatase nonreceptor type 11
-
Protein tyrosine phosphatase receptor-type T
-
-
protein tyrosine phosphatase SHP-1
-
-
protein tyrosine phosphatase, non-receptor type 1
-
protein tyrosine phosphatase, receptor-type, Z polypeptide 1
-
-
protein tyrosine phosphatase-1B
protein tyrosine phosphatase-2
-
-
protein tyrosine phosphatase-BL
-
-
Protein tyrosine phosphatase-NP
-
-
-
-
Protein-protein-tyrosine phosphatase HA2
-
-
-
-
protein-tyrosine phosphatase
Protein-tyrosine phosphatase 1B
Protein-tyrosine phosphatase 1C
-
-
-
-
Protein-tyrosine phosphatase 1E
-
-
-
-
Protein-tyrosine phosphatase 2C
-
-
-
-
Protein-tyrosine phosphatase 2E
-
-
-
-
Protein-tyrosine phosphatase 3CH134
-
-
-
-
Protein-tyrosine phosphatase CL100
-
-
-
-
Protein-tyrosine phosphatase D1
Protein-tyrosine phosphatase ERP
-
-
-
-
Protein-tyrosine phosphatase G1
-
-
-
-
Protein-tyrosine phosphatase H1
-
-
-
-
Protein-tyrosine phosphatase LC-PTP
-
-
-
-
Protein-tyrosine phosphatase MEG1
-
-
-
-
Protein-tyrosine phosphatase MEG2
-
-
-
-
Protein-tyrosine phosphatase P19
-
-
-
-
Protein-tyrosine phosphatase PCPTP1
-
-
-
-
Protein-tyrosine phosphatase pez
-
-
-
-
Protein-tyrosine phosphatase PTP-RL10
-
-
-
-
Protein-tyrosine phosphatase PTP36
-
-
-
-
Protein-tyrosine phosphatase PTPL1
-
-
-
-
Protein-tyrosine phosphatase striatum-enriched
-
-
-
-
Protein-tyrosine phosphatase SYP
-
-
-
-
Protein-tyrosine-phosphatase SL
-
-
-
-
Protein-tyrosine-phosphate phosphohydrolase
-
-
-
-
PTEN
-
-
PTEN phosphoprotein phosphatase
-
-
PTP IA-2beta
-
-
-
-
PTP nonreceptor type 2
-
PTP-1B
PTP-1C
-
-
-
-
PTP-1D
-
-
-
-
PTP-2C
-
-
-
-
PTP-BAS
PTP-BL
-
-
PTP-E1
-
-
-
-
PTP-eta
-
-
PTP-H1
-
-
-
-
PTP-HA2
-
-
-
-
PTP-MEG2
-
-
PTP-NP
-
-
-
-
PTP-PEST
PTP-phosphatase
-
-
PTP-SH2beta
-
-
-
-
PTP1
-
-
PTP1B
PTP1C
-
-
-
-
PTP1D
-
-
-
-
PTP1e
-
-
PTP2C
-
-
-
-
PTPalpha
PTPase YVH1
-
-
-
-
PTPase-MEG1
PTPase-MEG2
PTPB1
PTPbeta
PTPD1
PTPepsilon
-
PTPG1
-
-
-
-
PTPgamma
-
-
PTPH1
PTPL1
-
-
PTPMEG
-
-
PTPN11
PTPN14
PTPN20 variant 15
-
PTPN22
PTPN23
PTPN5
PTPN6
PTPN7
PTPNE6
-
-
-
-
PTPP
-
-
PTPRdelta
-
PTPRJ
PTPRomega
-
PTPRR
PTPRT
PTPRV
-
-
PTPRZ1
-
-
PY protein phosphatase
-
-
-
-
R-PTP-alpha
-
-
-
-
R-PTP-beta
-
-
-
-
R-PTP-delta
-
-
-
-
R-PTP-epsilon
-
-
-
-
R-PTP-eta
-
-
-
-
R-PTP-gamma
-
-
-
-
R-PTP-kappa
-
-
-
-
R-PTP-mu
-
-
-
-
R-PTP-zeta
-
-
-
-
receptor protein tyrosine phosphatase isoform delta
-
receptor protein tyrosine phosphatase isoform omega
-
receptor protein tyrosine phosphatase T
-
-
receptor protein tyrosine phosphatase {kappa}
-
-
receptor PTPepsilon
-
Receptor-linked protein-tyrosine phosphatase 10D
-
-
-
-
Receptor-linked protein-tyrosine phosphatase 99A
-
-
-
-
receptor-type protein tyrosine phosphatase J
-
-
Receptor-type protein-tyrosine phosphatase-kappa
-
-
receptor-type tyrosine-protein phosphatase B
-
receptor-type tyrosine-protein phosphatase R
UniProt
RNA/RNP complex-intereracting phosphatase
-
-
-
-
ROL B protein
-
-
-
-
RPTPalpha
RPTPdelta
-
RPTPgamma
-
RPTPkappa
RPTPlambda
-
RPTPsigma
-
Scr homology 2-containing tyrosine phosphatase
-
-
selective striatal enriched protein phosphatase
-
SH-PTP1
-
-
-
-
SH-PTP2
-
-
-
-
SH-PTP3
-
-
-
-
SH2 domain-containing tyrosine phosphatase-1
-
-
SH2 domain-containing tyrosine phosphatase-2
-
-
SHP
-
-
-
-
SHP-1
SHP-2
Small tyrosine phosphatase
-
-
-
-
Small, acidic phosphotyrosine protein phosphatase
-
-
-
-
SPH-1
-
-
SPH-2
-
-
Src homology region 2 domain-containing phosphatase 1
-
-
Src homology-2 domain containing protein tyrosine phosphatase-1
-
-
Src homology-2 domain containing protein tyrosine phosphatase-2
-
-
striatal-enriched PTP
-
-
String protein
-
-
-
-
Syp
-
-
-
-
T cell protein tyrosine phosphatase
-
-
T-cell protein tyrosine phosphatase
T-cell protein-tyrosine phosphatase
-
-
-
-
T-cell PTP
T-DSP11
-
-
-
-
T200
-
-
-
-
TC PTP
-
-
TC48
isoform
TCPTP
testis- and skeletal-muscle-specific DSP
-
-
testis- and skeletal-muscle-specific dual specificity protein phosphatase
-
-
Testis-and skeletal-muscle-specific DSP
-
-
-
-
TMDP
-
-
tyrosine O-phosphate phosphatase
-
-
-
-
tyrosine phosphatase
Tyrosine phosphatase CBPTP
-
-
-
-
tyrosine phosphatase IA-2
-
tyrosine phosphatase-1B
-
tyrosine-protein phosphatase non-receptor type 1
UniProt
tyrosine-protein phosphatase non-receptor type 5
UniProt
tyrosylprotein phosphatase
-
-
-
-
vaccinia H1-related PTP
-
[phosphotyrosine]protein phosphatase
-
-
-
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
[a protein]-tyrosine phosphate + H2O = [a protein]-tyrosine + phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of phosphoric ester
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
protein-tyrosine-phosphate phosphohydrolase
Dephosphorylates O-phosphotyrosine groups in phosphoproteins, such as the products of EC 2.7.10.2, non-specific protein-tyrosine kinase.
CAS REGISTRY NUMBER
COMMENTARY hide
79747-53-8
-
97162-86-2
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
Reversibility
r=reversible
ir=irreversible
?=not specified
3,6-fluorescein diphosphate + H2O
? + phosphate
show the reaction diagram
Substrates: -
Products: -
?
3-nitrobenzyl phosphate + H2O
3-nitrobenzyl alcohol + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
4-nitrophenyl phosphate + H2O
4-nitrophenol + phosphate
show the reaction diagram
4-nitrophenyl phosphate+ H2O
4-nitrophenol + phosphate
show the reaction diagram
4-nitrophenylphosphate + H2O
4-nitrophenol + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferol + phosphate
show the reaction diagram
6,8-difluoro-4-methylumbelliferyl phosphate + H2O
6,8-difluoro-4-methylumbelliferone + phosphate
show the reaction diagram
AAAAApYEEVH + H2O
AAAAAYEEVH + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
AAAAApYRHRR + H2O
AAAAAYRHRR + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
Ac-AAAApYAAAA-NH2 + H2O
Ac-AAAAYAAAA-NH2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-AAAEpYAAAA-NH2 + H2O
Ac-AAAEYAAAA-NH2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-AAAQpYAAAA-NH2 + H2O
Ac-AAAQYAAAA-NH2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
Ac-DGEEpYDDPF-NH2 + H2O
Ac-DGEEYDDPF-NH2 + phosphate
show the reaction diagram
-
Substrates: SKAP-HOM Tyr75 peptide
Products: -
?
Ac-ENDEpYTARE-NH2 + H2O
Ac-ENDEYTARE-NH2 + phosphate
show the reaction diagram
-
Substrates: Lck Tyr394 peptide
Products: -
?
Ac-TEPQpYQPGE-NH2 + H2O
Ac-TEPQYQPGE-NH2 + phosphate
show the reaction diagram
-
Substrates: Lck Tyr505 peptide
Products: -
?
Ac-YGEEpYDDLY-NH2 + H2O
Ac-YGEEYDDLY-NH2 + phosphate
show the reaction diagram
-
Substrates: consensus peptide 1
Products: -
?
Ac-YGYEpYDDEY-NH2 + H2O
Ac-YGYEYDDEY-NH2 + phosphate
show the reaction diagram
-
Substrates: consensus peptide 2
Products: -
?
acetyl-DADEpY-NH2 + H2O
acetyl-DADEY-NH2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
acetyl-DADEpYL-NH2 + H2O
acetyl-DADEYL-NH2 + phosphate
show the reaction diagram
Substrates: -
Products: -
?
ADEDFpYAA + H2O
ADEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
AKFEDTpYAA + H2O
AKFEDTYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1
Products: -
?
angiotensin I + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
ARKRIpYAA + H2O
ARKRIYAA + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
ASSDDpYAA + H2O
ASSDDYAA + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
AVWEFpYpYAA + H2O
? + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1
Products: -
?
AWSpYADpYAA + H2O
? + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1
Products: -
?
AYTEpYTpYAA + H2O
? + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1
Products: -
?
bis(4-nitrophenyl) phosphate + H2O
?
show the reaction diagram
Substrates: -
Products: -
?
bis-(p-phosphophenyl) methane + H2O
?
show the reaction diagram
Substrates: synthetic high-affinity low-molecular weight nonpeptide substrate
Products: -
?
bovine serum albumin + H2O
? + phosphate
show the reaction diagram
carrier protein-Cdc2-phosphotyrosine + H2O
carrier protein-Cdc2-tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
carrier protein-Y3-phosphotyrosine + H2O
carrier protein-Y3-tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
carrier protein-Y5-phosphotyrosine + H2O
carrier protein-Y5-tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
Cdk2-pTpY + H2O
Cdk2-TpY + phosphate
show the reaction diagram
-
Substrates: dephosphorylates Cdk/cyclins on pThr14 and/or pTyr15 residues
Products: -
?
Cdk2-pTpY/CycA + H2O
Cdk2-pTY/CycA + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
DADEpYIPQQG + H2O
DADEYIPQQG + phosphate
show the reaction diagram
-
Substrates: specific substrate for PTP1B
Products: -
?
DADEpYLIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
DAEDFpYAA + H2O
DAEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
DDT-(3,5-difluoro)YDpYAA + H2O
DDT-(3,5-difluoro)YDYAA + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
DDTYDpYAA + H2O
DDTYDYAA + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
DFEDFpYAA + H2O
DFEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
difluoromethylumbelliferyl phosphate + H2O
difluoromethylumbelliferone + phosphate
show the reaction diagram
Substrates: -
Products: -
?
DNL-(3,5-difluoro)YpYWD + H2O
DNL-(3,5-difluoro)YYWD + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
DNLYpYWD + H2O
DNLYYWD + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
DWEDFpYAA + H2O
DWEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
EADTApYAA + H2O
EADTAYAA + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
EIFDFpYAA + H2O
EIFDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
ENDpYINASL + H2O
ENDYINASL + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
ENPE(pY)LGLD + H2O
ENPEYLGLD + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1248
Products: -
?
ENPE(pY)LTPQ + H2O
ENPEYLTPQ + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1196
Products: -
?
EphA3-phosphotyrosine + H2O
EphA3-tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
epidermal growth factor + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
epidermal growth factor receptor + H2O
? + phosphate
show the reaction diagram
-
Substrates: with phosphotyrosine Tyr992
Products: -
?
FDEDFpYAA + H2O
FDEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
FDIDIpYAA + H2O
FDIDIYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
FDNL(pY)2WDQD + H2O
FDNLYYWDQD + 2 phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1221/1222
Products: -
?
fluorescein diphosphate + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
fluorescein diphosphate + H2O
fluorescein phosphate + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
FYDIDpYAA + H2O
FYDIDYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
Gab1 tyrosine phosphate + H2O
Gab1 tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
GESDGGpYMDMSKD + H2O
GESDGGYMDMSKD + phosphate
show the reaction diagram
-
Substrates: this peptide corresponds to the sequence containing Tyr740 of the human platelet-derived growth factor receptor
Products: -
?
GNGDpYMPMSPKS + H2O
GNGDYMPMSPKS + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
human A431 membrane protein + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
insulin receptor phosphopeptide + H2O
insulin receptor peptide + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
insulin-like growth factor-1 + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
LDEpYVATR + H2O
LDEYVATR + phosphate
show the reaction diagram
Substrates: -
Products: -
?
LIEDNEpYTARQGA + H2O
LIEDNEYTARQGA + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
lysozyme + H2O
? + phosphate
show the reaction diagram
-
Substrates: reduced, carboxymethylated and maleylated
Products: -
?
membrane protein 3 + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
myelin basic protein + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
myosin P-light chain + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
n-nitrophenyl phosphate + H2O
n-nitrophenol + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
O-phospho-L-tyrosine + H2O
tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
p-nitrophenyl phosphate
p-nitrophenol + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
p-nitrophenyl phosphate + H2O
p-nitrophenol + phosphate
show the reaction diagram
p38 + H2O
?
show the reaction diagram
paxilin tyrosine phosphate + H2O
paxilin tyrosine + phosphate
show the reaction diagram
PGSAAP-pY-LKTKFI + H2O
PGSAAPYLKTKFI + phosphate
show the reaction diagram
Substrates: STAT3 peptide
Products: -
?
phosphocaveolin-1 + H2O
caveolin-1 + phosphate
show the reaction diagram
-
Substrates: phosphorylated at Y14
Products: -
?
phosphorylated actin + H2O
actin + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated adenomatous Polyposis coli-protein + H2O
adenomatous Polyposis coli-protein + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated alpha-actinin + H2O
alpha-actinin + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated BCR-Abl + H2O
BCR-Abl + phosphate
show the reaction diagram
Substrates: -
Products: -
?
phosphorylated c-MET + H2O
c-MET + phosphate
show the reaction diagram
phosphorylated CD3 epsilon + H2O
CD3 epsilon + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Cdk2-pTpY/CycA protein + H2O
Cdk2-pTpY/CycA protein + phosphate
show the reaction diagram
Substrates: -
Products: -
?
phosphorylated EphA2 receptor + H2O
EphA2 receptor + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated EphA5 + H2O
EphA5 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
show the reaction diagram
phosphorylated ErbB1 + H2O
ErbB1 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated ErbB2 + H2O
ErbB2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated ERK1 + H2O
ERK1 + phosphate
show the reaction diagram
Substrates: -
Products: -
?
phosphorylated ERK2 + H2O
ERK2 + phosphate
show the reaction diagram
Substrates: HePTP binds the phosphorylated tyrosine of the Erk2 peptide (pY185), Erk2 residue T183, which is phosphorylated in maximally activated Erk2, is not essential for substrate recognition and binding by HePTP
Products: -
?
phosphorylated extracellular signal regulated kinase + H2O
extracellular signal regulated kinase + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Ezrin + H2O
Ezrin + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated focal adhesion kinase + H2O
focal adhesion kinase + phosphate
show the reaction diagram
-
Substrates: dephosphorylation occurs at Tyr-397, PTPD1 activity is required for focal adhesion kinase autophosphorylation and adhesion plaque stability
Products: -
?
phosphorylated IGF-I receptor + H2O
IGF-I receptor + phosphate
show the reaction diagram
-
Substrates: isozyme p52shc
Products: -
?
phosphorylated insulin receptor + H2O
insulin receptor + phosphate
show the reaction diagram
phosphorylated JAK2 + H2O
JAK2 + phosphate
show the reaction diagram
-
Substrates: SHP2 dephosphorylates the Tyr1007 site, preventing the formation of the JAK2-Socs1 complex
Products: -
?
phosphorylated Janus kinase 2 + H2O
Janus kinase 2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated JNK + H2O
JNK + phosphate
show the reaction diagram
Substrates: -
Products: -
?
phosphorylated Jun amino-terminal kinase + H2O
Jun amino-terminal kinase + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Lck + H2O
Lck + phosphate
show the reaction diagram
-
Substrates: component of the T cell receptor signaling pathway
Products: -
?
phosphorylated Munc18c + H2O
Munc18c + phosphate
show the reaction diagram
-
Substrates: dephosphorylation at Tyr218/219 and Tyr521
Products: -
?
phosphorylated p130 Crk-associated substrate + H2O
p130 Crk-associated substrate + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated p38 mitogen-activated protein kinase + H2O
p38 mitogen-activated protein kinase + phosphate
show the reaction diagram
phosphorylated phospholipase Cgamma + H2O
phospholipase Cgamma + phosphate
show the reaction diagram
-
Substrates: dephosphorylation occurs at Tyr-783
Products: -
?
phosphorylated platelet-derived growth factor receptor + H2O
platelet-derived growth factor receptor + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated protein kinase-like endoplasmic reticulum kinase + H2O
protein kinase-like endoplasmic reticulum kinase + phosphate
show the reaction diagram
-
Substrates: dephosphorylation at Tyr615
Products: -
?
phosphorylated protein p85
protein p85 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated pyruvate kinase M2 + H2O
pyruvate kinase M2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated RET(C634R) oncoprotein + H2O
RET(C634R) oncoprotein + phosphate
show the reaction diagram
-
Substrates: dephosphorylation at Tyr905 and Tyr1062
Products: -
?
phosphorylated RET-MEN2A oncoprotein + H2O
RET-MEN2A oncoprotein + phosphate
show the reaction diagram
-
Substrates: dephosphorylation at Tyr905 and Tyr1062
Products: -
?
phosphorylated RET/PTC1 oncoprotein + H2O
RET/PTC1 oncoprotein + phosphate
show the reaction diagram
-
Substrates: dephosphorylation at Tyr905 and Tyr1062
Products: -
?
phosphorylated signal transducer and activator of transcription 3 + H2O
signal transducer and activator of transcription 3 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Src + H2O
Src + phosphate
show the reaction diagram
phosphorylated Src protein + H2O
Src protein + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Src tyrosine kinase + H2O
Src tyrosine kinase + phosphate
show the reaction diagram
-
Substrates: PTPD1 associates with and activates Src tyrosine kinase
Products: -
?
phosphorylated STAT1 + H2O
STAT1 + phosphate
show the reaction diagram
phosphorylated STAT3 + H2O
STAT3 + phosphate
show the reaction diagram
phosphorylated STAT5 + H2O
STAT5 + phosphate
show the reaction diagram
-
Substrates: purified SHP2 protein directly dephosphorylates STAT5 or tyrosine-phosphorylated peptides derived from STAT5
Products: -
?
phosphorylated T cell antigen receptor zeta + H2O
T cell antigen receptor zeta + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated valosin containing protein + H2O
valosin containing protein + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated vascular endothelial growth factor receptor 2 + H2O
vascular endothelial growth factor receptor 2 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Vav + H2O
Vav + phosphate
show the reaction diagram
-
Substrates: component of the T cell receptor signaling pathway
Products: -
?
phosphorylated ZAP-70 + H2O
ZAP-70 + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Zap70 + H2O
Zap70 + phosphate
show the reaction diagram
-
Substrates: protein-tyrosine kinase
Products: -
?
phosphothreonine + H2O
threonine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphotyrosine + H2O
tyrosine + phosphate
show the reaction diagram
phosphotyrosine serum albumin + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphotyrosyl bovine serum albumin + H2O
tyrosyl-bovine serum albumin + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphotyrosyl-casein + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphotyrosyl-STAT3 + H2O
STAT3 + phosphate
show the reaction diagram
platelet-derived growth factor receptor + H2O
? + phosphate
show the reaction diagram
PLC-gamma1 tyrosine phosphate + H2O
PLC-gamma1 tyrosine + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
PLQR(pY)SEDP + H2O
PLQRYSEDP + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1112
Products: -
?
poly(Glu,Tyr) + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
PQDKEY-pY-KVKEPG + H2O
PQDKEYYKVKEPG + phosphate
show the reaction diagram
Substrates: JAK2 peptide
Products: -
?
protein FAK + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
protein Shc + H2O
?
show the reaction diagram
-
Substrates: -
Products: -
?
RE-(3,5-difluoro)YEFpYAA + H2O
RE-(3,5-difluoro)YEFYAA + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
REYEFpYAA + H2O
REYEFYAA + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
RKGSGD-pY-MPMSPK + H2O
RKGSGDYMPMSPK + phosphate
show the reaction diagram
Substrates: IRS1 peptide
Products: -
?
RRISTpYAA + H2O
RRISTYAA + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
RRLIEDAEpYAARG + H2O
RRLIEDAEYAARG + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
SASASpYDWEF + H2O
SASASYDWEF + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
SASASpYSASA + H2O
SASASYSASA + phosphate
show the reaction diagram
SKAP-HOM + H2O
?
show the reaction diagram
-
Substrates: a cytosolic adaptor protein required for proper activation of the immune system, a bona fide Lyp substrate
Products: -
?
soluble N-ethylmaleimide-sensitive factor attachment protein receptor + H2O
soluble N-ethylmaleimide-sensitive factor attachment protein receptor + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
TATEPQpYQPGEN + H2O
TATEPQYQPGEN + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
TATEPQpYQPGENL + H2O
TATEPQYQPGENL + phosphate
show the reaction diagram
-
Substrates: substrate of RPTPalpha
Products: -
?
TGFLTELpYVATRWY + H2O
TGFLTELYVATRWY + phosphate
show the reaction diagram
-
Substrates: this peptide corresponds to the sequence containing Tyr204 of the human extracellular signal-regulated kinase
Products: -
?
TSTEPQpYQPGENL + H2O
TSTEPQYQPGENL + phosphate
show the reaction diagram
tyrosin kinase + H2O
? + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
WAGDDpYAA + H2O
WAGDDYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
WDEDFpYAA + H2O
WDEDFYAA + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-2
Products: -
?
WDEDFpYDWEF + H2O
WDEDFYDWEF + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
WDEDFpYRWKF + H2O
WDEDFYRWKF + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
WDEDFpYSASA + H2O
WDEDFYSASA + phosphate
show the reaction diagram
WRKRFpYDWEF + H2O
WRKRFYDWEF + phosphate
show the reaction diagram
-
Substrates: substrate of SHP-1 and SHP-2
Products: -
?
Y527-phosphorylated Src + H2O
Src + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
YCRPESQEHPEADPGAAPpYLK + H2O
YCRPESQEHPEADPGAAYLK + phosphate
show the reaction diagram
-
Substrates: YCRPESQEHPEADPGAApYLK is signal transducer and activator of transcription 3, is dephosphorylated at Y705
Products: -
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
show the reaction diagram
[epidermal growth factor receptor 2]-tyrosine phosphate + H2O
[epidermal growth factor receptor 2]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation of epidermal growth factor receptor 2 (HER2)-pY1196 site
Products: -
?
[epidermal growth factor receptor]-tyrosine phosphate + H2O
[epidermal growth factor receptor]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[Eps15 peptide846-854 P850V]-tyrosine phosphate + H2O
[Eps15 peptide846-854 P850V]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[Eps15 peptide846-854]-tyrosine phosphate + H2O
[Eps15 peptide846-854]-tyrosine + phosphate
show the reaction diagram
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
show the reaction diagram
[ERK1]-tyrosine phosphate + H2O
[ERK1]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[ERK2]-tyrosine phosphate + H2O
[ERK2]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[FAK]-tyrosine phosphate + H2O
[FAK]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr397
Products: -
?
[FYN kinase]-tyrosine phosphate + H2O
[FYN kinase]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[HER2]-tyrosine phosphate + H2O
[HER2]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1112, Tyr1196, Tyr1221, Tyr1222, and Tyr1248
Products: -
?
[insulin receptor kinase]-tyrosine phosphate + H2O
[insulin receptor kinase]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[p130Cas]-tyrosine phosphate + H2O
[p130Cas]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr165
Products: -
?
[p190RhoGAP]-tyrosine phosphate + H2O
[p190RhoGAP]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr1105
Products: -
?
[paxillin]-tyrosine phosphate + H2O
[paxillin]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr118
Products: -
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[SRC]-tyrosine phosphate + H2O
[SRC]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr416
Products: -
?
[VAV2]-tyrosine phosphate + H2O
[VAV2]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation at Tyr172
Products: -
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
DADE(pY)LIPQQG + H2O
DADEYLIPQQG + phosphate
show the reaction diagram
Substrates: a physiological phosphopeptide substrate of enzyme PTP1B
Products: -
?
paxilin tyrosine phosphate + H2O
paxilin tyrosine + phosphate
show the reaction diagram
-
Substrates: PTPRT specifically regulates paxillin phosphorylation at Tyr88 in colorectal cancer cells
Products: -
?
phosphocaveolin-1 + H2O
caveolin-1 + phosphate
show the reaction diagram
-
Substrates: phosphorylated at Y14
Products: -
?
phosphorylated alpha-actinin + H2O
alpha-actinin + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated CD3 epsilon + H2O
CD3 epsilon + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated epidermal growth factor receptor + H2O
epidermal growth factor receptor + phosphate
show the reaction diagram
-
Substrates: inactivation of EGFR
Products: -
?
phosphorylated IGF-I receptor + H2O
IGF-I receptor + phosphate
show the reaction diagram
-
Substrates: isozyme p52shc
Products: -
?
phosphorylated Lck + H2O
Lck + phosphate
show the reaction diagram
-
Substrates: component of the T cell receptor signaling pathway
Products: -
?
phosphorylated p130 Crk-associated substrate + H2O
p130 Crk-associated substrate + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated T cell antigen receptor zeta + H2O
T cell antigen receptor zeta + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated valosin containing protein + H2O
valosin containing protein + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
phosphorylated Vav + H2O
Vav + phosphate
show the reaction diagram
-
Substrates: component of the T cell receptor signaling pathway
Products: -
?
phosphorylated Zap70 + H2O
Zap70 + phosphate
show the reaction diagram
-
Substrates: protein-tyrosine kinase
Products: -
?
phosphotyrosyl-STAT3 + H2O
STAT3 + phosphate
show the reaction diagram
-
Substrates: signal transducers and activator of transcription 3, STAT3, is a transcription factor that is associated with survival, proliferation, chemoresistance, and angiogenesis of tumor cells
Products: -
?
Y527-phosphorylated Src + H2O
Src + phosphate
show the reaction diagram
-
Substrates: -
Products: -
?
[a protein]-tyrosine phosphate + H2O
[a protein]-tyrosine + phosphate
show the reaction diagram
[epidermal growth factor receptor 2]-tyrosine phosphate + H2O
[epidermal growth factor receptor 2]-tyrosine + phosphate
show the reaction diagram
Substrates: dephosphorylation of epidermal growth factor receptor 2 (HER2)-pY1196 site
Products: -
?
[Eps15 peptide]-tyrosine phosphate + H2O
[Eps15 peptide]-tyrosine + phosphate
show the reaction diagram
[ERK1]-tyrosine phosphate + H2O
[ERK1]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[ERK2]-tyrosine phosphate + H2O
[ERK2]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[FYN kinase]-tyrosine phosphate + H2O
[FYN kinase]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[insulin receptor kinase]-tyrosine phosphate + H2O
[insulin receptor kinase]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
[protein]-tyrosine phosphate + H2O
[protein]-tyrosine + phosphate
show the reaction diagram
Substrates: -
Products: -
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
NaF
-
activation
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
((1E)-2-nitroprop-1-en-1-yl)benzene
-
50% inhibition at 0.023 mM in absence of 2-mercaptoethanol, at 0.515 mM in presence of 1 mM 2-mercaptoethanol
((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate
50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F
((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F
((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate)
50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F
((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate
50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate
50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F
((4-((4E)-2-(1H-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonic acid
-
50% inhibition at 109 nM for isoform PTP-1B, at 95 nM for isoform TCPTP
((E)-2-nitrovinyl)benzene
-
i.e. trans-beta-nitrostyrene, slow-binding inhibitor, acting as a pY mimetic and binding to the enzyme active site to form an initial noncovalent E*I complex, followed by nucleophilic attack on the nitrostyrene nitro group by C215 of enzyme to form a reversible, covalent adduct. 50% inhibition at 0.0025 mM in absence of 2-mercaptoethanol, at 0.4 mM in presence of 1 mM 2-mercaptoethanol
(1-benzyl-3-methyl-2,3-dihydro-1H-imidazol-2-yl)(chloro)gold
-
i.e. [(BzMeIm)AuICl]
(1R,3aS,3bS,10aR,10bS,12aR)-1-[(2R)-4-carboxybutan-2-yl]-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-9-carboxylic acid
-
-
(1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate
no inhibition at 0.021 mM
(1S,3aR,8S,8aS,8bR)-4-henicosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,5a,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(1S,3aS,4R,8S,8aS,8bR)-4-icosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,4,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(2,3-dibromo-4,5-dihydroxyphenyl)(2,3,6-tribromo-4,5-dihydroxyphenyl)methanone
a competitive PTP1B inhibitor by Lineweaver-Burk analysis, 95.07% inhibition at 0.02 mg/ml
(2,3-dibromo-4,5-dimethoxyphenyl)(2,3,6-tribromo-4,5-dimethoxyphenyl)methanone
(2alpha,3alpha)-2,3-dihydroxyolean-12-en-28-oic acid
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-2a-(hydroxymethyl)-3-icosyl-6a,7a-dimethyl-2a,3,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2,5-dione
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-3-icosyl-6a,7a-dimethyl-2,5-dioxo-3,5,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2a(2H)-carbaldehyde
-
-
(2beta,3beta)-2,3-dihydroxyolean-12-en-28-oic acid
-
-
(2E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-1-(3-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(4-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-[3-(benzyloxy)phenyl]-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-(5-bromo-2,4-dihydroxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-[[(methoxycarbonyl)sulfanyl]amino]phenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-butoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(3-methylbut-3-en-2-yl)-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(1H-pyrazol-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(methylsulfonyl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(4-methylphenyl)sulfonyl]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)-1,3-benzodioxol-5-yl]prop-2-en-1-one
-
-
(2E)-3-phenylprop-2-enoic acid
-
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-5-(3-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[5-bromo-2-hydroxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-[5-bromo-2-methoxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2R)-2-benzyl-3-[2,6-dibromo-4-(6-bromo-5a,11a-dihydrobenzo[b]naphtho[2,3-d]furan-11-yl)phenyl]propanoic acid
-
(2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
-
(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
-
(3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate
no inhibition at 0.020 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate
no inhibition at 0.025 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate
no inhibition at 0.024 mM
(3beta)-3-(acetyloxy)olean-12-en-28-oic acid
-
-
(3beta)-3-hydroxyolean-12-en-28-oic acid
-
-
(3beta)-3-hydroxyoleana-11,13(18)-dien-28-oic acid
-
-
(3S,3aR,4S,5R,7aR)-4-acetyl-7-henicosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,5,7a-hexahydro-2-benzofuran-5-carboxylic acid
-
-
(3S,3aR,4S,7R,7aS)-4-acetyl-7-icosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,7,7a-hexahydro-2-benzofuran-5-carboxylic acid
-
-
(4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate
50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F
(4aR,6aR,6bS,8aR,12aS,14aR,14bR)-8a-hydroxy-4,4,6a,6b,11,11,14b-heptamethyl-1,4a,5,6,6a,6b,7,8a,9,10,11,12,12a,14,14a,14b-hexadecahydropicene-3,8(2H,4H)-dione
-
-
(4aR,6aS,6bR,8aR,10S,12aR,12bR,14bS)-4a,10-dihydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicen-5(1H)-one
-
-
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-11-(methylamino)-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,6a,9a,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d][1,2]oxazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
competitive PTP1B inhibitor
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,8,11a,13a-pentamethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
-
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(6aS,6bR,8aR,10S,12aS,12bR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b-hexadecahydropicen-5(1H)-one
-
-
(7bS,9R,13bR,15R)-7-amino-9-(hydroxymethyl)-10,13-dioxo-2,3,3a,3b,4,5,6,7,7a,7b,9,10,13,13b-tetradecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-15-carbonitrile
inhibits Cdc25B modestly
(7bS,9R,13bR,15S)-7-amino-15-hydroxy-9-(hydroxymethyl)-2,3,3a,3b,4,5,6,7,7a,7b,9,13b-dodecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-10,13-dione
-
(difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid
-
50% inhibition at 163 nM for PTP-1B wild-type, at 1903 nM for PTP-1B mutant L119V, and at 1600 nM for isoform TCPTP wild-type and 138 nM for TCPTP mutant V121L
(E)-1-[4-(1H-pyrazol-1-yl)phenyl]-3-(5-allyl-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
(E)-2-(4-(3-(5-allyl-2-methoxy-4-[(tetrahydro-2H-pyran-2-yl)oxy]phenyl)acryloyl)phenoxy)acetic acid
-
-
(E)-2-[4-[3-[5-allyl-2-methoxy-4-[(tetrahydro-2H-pyran-2-yl)oxy]phenyl]acryloyl]phenoxy]acetic acid
-
(E)-3-(5-allyl-2-methoxy-4-[(tetrahydro-2H-pyran-2-yl)oxy]phenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(E)-3-(5-allyl-2-methoxy-4-[(tetrahydro-2H-pyran-2-yl)oxy]phenyl)-1-[4-(allyloxy)-2-hydroxyphenyl]prop-2-en-1-one
-
-
(E)-3-(5-allyl-4-hydroxy-2-isopropoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(2-hydroxy-4-methoxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]phenyl)prop-2-en-1-one
-
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(3-allyl-4-methoxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(3-hydroxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(4-ethoxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(4-morpholinophenyl)prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-(4-[(3-methylbut-2-en-1-yl)oxy]phenyl)prop-2-en-1-one
-
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[3-(diallylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(allyloxy)-2-hydroxyphenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(allyloxy)-2-methoxyphenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(allyloxy)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(diallylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
(E)-3-(5-allyl-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)benzo[d][1,3]dioxol-5-yl]prop-2-en-1-one
-
(E)-3-[5-allyl-2-methoxy-4-[(tetrahydro-2H-pyran-2-yl)oxy]phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
(E)-4-(4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy)butanoic acid
-
-
(E)-4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenyl-4-(tert-butyl)benzoate
-
(E)-4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenyl-4-bromobenzoate
-
(E)-4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenylbenzoate
-
(E)-4-[4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy]butanoic acid
-
(E)-5-(4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy)pentanoic acid
-
-
(E)-5-[4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy]pentanoic acid
-
(E)-ethyl 2-(4-[3-(5-allyl-hydroxy-2-methoxyphenyl)acryloyl]phenoxy)acetate
-
-
(E)-ethyl 2-[4-[3-(5-allyl-hydroxy-2-methoxyphenyl)acryloyl]phenoxy]acetate
-
(E)-ethyl 5-(4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy)pentanoate
-
-
(E)-ethyl 5-[4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy]pentanoate
-
(E)-ethyl4-(4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy)butanoate
-
-
(E)-ethyl4-[4-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenoxy]butanoate
-
(E)-N-(3-[3-(5-allyl-4-hydroxy-2-methoxyphenyl)acryloyl]phenyl)methanesulfonamide
-
-
(E)-N-(4,5-diphenyl-1,3-thiazol-2-yl)-2-naphthalen-2-ylethenesulfonamide
-
(E)-N-[4-(4-chlorophenyl)-5-propyl-1,3-thiazol-2-yl]-2-(3,4-dichlorophenyl)ethenesulfonamide
-
(Z)-1-(3-(3-carboxy-3-hydroxyacryloyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 2.4 mg/ml
(Z)-1-(3-(4-ethoxy-3-hydroxy-4-oxobut-2-enoyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 3.1 mg/ml
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
-
NSC-117199
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
-
-
(Z)-5-(2,3-dibromo-4,5-dimethoxybenzylidene)thiazolidine-2,4-dione
95.95% inhibition at 0.02 mg/ml
(Z)-5-(2,3-dibromo-4-hydroxy-5-methoxybenzylidene)thiazolidine-2,4-dione
35.22% inhibition at 0.02 mg/ml
(Z)-5-(2-bromo-3,4-dimethoxybenzylidene)imidazolidine-2,4-dione
19.78% inhibition at 0.02 mg/ml
(Z)-5-(2-bromo-3,4-dimethoxybenzylidene)thiazolidine-2,4-dione
14.94% inhibition at 0.02 mg/ml
(Z)-5-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxybenzylidene)thiazolidine-2,4-dione
95.72% inhibition at 0.02 mg/ml. The compound enhances the insulin-stimulated phosphorylation of IRbeta, IRS-1 and Akt in C2C12 myotubes. (Z)-5-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxybenzylidene)thiazolidine-2,4-dione increases liver glycogen storage and improves islet architecture with more beta-cells and fewer alpha-cells in dia
(Z)-5-(3-bromo-4,5-dihydroxybenzylidene)thiazolidine-2,4-dione
98.82% inhibition at 0.02 mg/ml
(Z)-5-(3-bromo-4,5-dimethoxybenzylidene)imidazolidine-2,4-dione
12.08% inhibition at 0.02 mg/ml
(Z)-5-(3-bromo-4-hydroxy-5-methoxybenzylidene)imidazolidine-2,4-dione
(Z)-5-(3-bromo-4-hydroxy-5-methoxybenzylidene)thiazolidine-2,4-dione
47.51% inhibition at 0.02 mg/ml
(Z)-5-(4-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxyphenoxy)benzylidene)thiazolidine-2,4-dione
93.39% inhibition at 0.02 mg/ml
(Z)-5-(4-hydroxy-3-methoxybenzylidene)imidazolidine-2,4-dione
28.67% inhibition at 0.02 mg/ml
(Z)-5-(4-hydroxy-3-methoxybenzylidene)thiazolidine-2,4-dione
([2-bromo-4-(3-oxo-2,3-diphenylpropyl)phenyl](difluoro)methyl)phosphonic acid
-
1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
-
-
1,1'-methylenebis(2,3,6-tribromo-4,5-dimethoxybenzene)
complete inhibition at 0.02 mg/ml
1,2,4-tribromo-3-[(2,3-dibromo-4,5-dimethoxyphenyl)methyl]-5,6-dimethoxybenzene
1,3-difluoro-2-[(E)-2-nitroethenyl]benzene
-
50% inhibition at 0.0048 mM in absence of 2-mercaptoethanol, at 0.34 mM in presence of 1 mM 2-mercaptoethanol
1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1-(1,3-benzodioxol-5-yl)-2-([1-(4-hydroxyphenyl)-1H-1,2,3,4-tetraazol-5-yl]sulfanyl)-1-ethanone
88% inhibition at 0.2 mM
1-(2,6-dihydroxy-4-methoxy-3-methylphenyl)ethanone
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
36.2% inhibition at 0.02 mg/ml
1-(4-hydroxy-3-(methoxycarbonyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 8.1 mg/ml
1-benzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1-benzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.1% inhibition at 0.02 mg/ml
1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.7% inhibition at 0.02 mg/ml
1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.8% inhibition at 0.02 mg/ml
1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.5% inhibition at 0.02 mg/ml
1-cyclopropyl-N-(4-fluorobenzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
3.3% inhibition at 0.02 mg/ml
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
-
covalent mode of action
1-heptyl-1H-imidazol-4-yl)-7-hydroxy-4H-chromen-4-one
-
1-methoxy-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.0045 mM in absence of 2-mercaptoethanol, at 0.27 mM in presence of 1 mM 2-mercaptoethanol
1-methyl-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.003 mM in absence of 2-mercaptoethanol, at 0.225 mM in presence of 1 mM 2-mercaptoethanol
1-phenyl-1H-pyrrole-2,5-dione
-
1-[7-methyl-3-(trifluoromethyl)naphthalen-1-yl]piperazine
DES-4884, a piperazinylquinoline fragment, binds to pocket 2, which overlaps with the allosteric pocket, enzyme binding structure, crystal structure analysis (PDB ID 8G67)
15-hydroxykaur-9(11),16-dien-19-oic acid
-
16alphaH,17-isovaleryloxy-ent-kauran-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.007 mM, noncompetitive
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid
-
-
2',4'-dihydroxy-1,1'-biphenyl
-
2,2'-[benzene-1,4-diylbis(methanediyloxybenzene-4,1-diyl)]bis(oxoacetic acid)
-
-
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
-
competitive, noncovalent mode of action
2,3-dibromo-1-[(2-bromo-3,4-dimethoxy-6-methylphenyl)methyl]-4,5-dimethoxybenzene
87.52% inhibition at 0.02 mg/ml
2,4-dihydroxy-6-methylbenzoic acid
-
45% inhibition of PTPB1 at 0.178 mM
2,4-dimethoxy-1-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.028 mM in absence of 2-mercaptoethanol, at 0.390 mM in presence of 1 mM 2-mercaptoethanol
2,5-dihydroxy-3-[7-(2-methylbenzyl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2,5-dihydroxy-3-[7-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2-((5-(naphthalen-1-yloxy)-1H-benzimidazol-1-yl)thio)-N-(thiazol-2-yl)acetamide
-
2-((5-(naphthalen-2-yloxy)-1H-benzimidazol-1-yl)thio)-N-(thiazol-2-yl)acetamide
-
2-((6-chloro-5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)-N-(thiazol-2-yl)acetamide
-
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
i.e. OATP
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-(1-(2,4-dichlorobenzyl)-1H-imidazol-2-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(2,4-dichlorobenzyl)-1H-imidazol-4-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(2,4-dichlorobenzyl)-1H-imidazol-5-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(3-chlorobenzyl)-1H-imidazol-2-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(3-chlorobenzyl)-1H-imidazol-4-yl)-7-hydroxy-4H-chromen-4-one
competitive inhibitor, the compound shows selectivity ratio (9.5fold) over T-cell protein tyrosine phosphatase (TCPTP). It is cell permeable with relatively low cytotoxicity
2-(1-(3-chlorobenzyl)-1H-imidazol-5-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-chlorobenzyl)-1H-imidazol-2-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-chlorobenzyl)-1H-imidazol-4-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-chlorobenzyl)-1H-imidazol-5-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-fluorobenzyl)-1H-imidazol-2-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-fluorobenzyl)-1H-imidazol-4-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-(4-fluorobenzyl)-1H-imidazol-5-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-heptyl-1H-imidazol-2-yl)-7-hydroxy-4H-chromen-4-one
-
2-(1-heptyl-1H-imidazol-5-yl)-7-hydroxy-4H-chromen-4-one
-
2-(2,5-dimethyl-1H-pyrrol-1-yl)-5-hydroxybenzoic acid
2-(2-((5-(naphthalen-1-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoic acid
-
2-(2-chloroacetamido)benzoic acid
-
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid
-
2-(oxalyl-amino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
-
2-bromo-N-phenylacetamide
-
2-carboperoxybenzoate
-
complete inhibition at 150 mM
2-chloro-1-(3,4-dihydroquinolin-1(2H)-yl)ethan-1-one
-
2-chloro-1-(4-phenylpiperazin-1-yl)ethan-1-one
-
2-chloro-4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
2-chloro-5-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
2-chloro-N-(1,2-oxazol-3-yl)acetamide
-
2-chloro-N-(1,3-thiazol-2-yl)acetamide
-
2-chloro-N-(2,3-dihydro-1,2-benzoxazol-3-yl)acetamide
-
2-chloro-N-(2-hydroxyphenyl)acetamide
-
2-chloro-N-(2-phenylethyl)acetamide
-
2-chloro-N-(4-phenyl-1,2-oxazol-5-yl)acetamide
-
2-chloro-N-(naphthalen-1-yl)acetamide
-
2-chloro-N-cyclohexylacetamide
-
2-chloro-N-phenylacetamide
-
2-chloro-N-[3-(4-chlorophenyl)-1,2-oxazol-5-yl]acetamide
-
2-chloro-N-[3-(4-methoxyphenyl)-1,2-oxazol-5-yl]acetamide
-
2-chloro-N-[3-(4-methylphenyl)-1,2-oxazol-5-yl]acetamide
-
2-chloro-N-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]acetamide
modeling of PTP1B bound to the compound
2-chloro-N-[4-(4-hydroxyphenyl)-1,3-thiazol-2-yl]acetamide
-
2-chloro-N-[5-(4-fluorophenyl)-1,2-oxazol-3-yl]acetamide
-
2-hydroperoxytetrahydrofuran
-
inactivation by 2-hydroperoxytetrahydrofuran (0.05 mM, 10 min) is reversed upon reaction of the enzyme with dithiothreitol (54% return of activity, following treatment with 100 mM dthiothreitol for 1 h)
2-iodo-N-phenylacetamide
-
2-phenyloxirane
-
2-[(4-[2-acetamido-3-[(5-[[(1S)-1-carboxy-3-(methylsulfanyl)propyl]amino]-5-oxopentyl)amino]-3-oxopropyl]-2-ethylphenyl)(oxalo)amino]benzoic acid
-
2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
i.e. TCS401, binds to the active site
2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-6-hydroxy-3-oxo-3H-xanthen-9-yl]benzoic acid
i.e. FlAsH
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
mixed-type inhibition, 99% inhibition at 0.2 mM
24-hydroxyursolic acid
-
-
28-(10-decanoic)-oleanolic acid
-
28-(12-dodecanoic)-oleanolic acid
-
28-(2-acetic)-oleanolic acid
-
28-(4-butyric)-oleanolic acid
-
28-(6-hexanoic)-oleanolic acid
-
28-(8-octanoic)-oleanolic acid
-
28-(glycine)-oleanolic acid amide
-
28-(L-glutamic acid)-oleanolic acid amide
-
28-(L-phenylalanine)-oleanolic acid amide
-
28-(p-carboxyphenyl)-oleanolic acid amide
-
28-[4-butyric((R)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-3-indole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-5-imidazole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-methylthioethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-2,3-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-oxymethyleneoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,5-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-fluorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-nitrophenylethyl)-amide]-DELTA12-oleanene
-
2alpha,3alpha,19alpha,23-tetrahydroxyurs-12-en-28-oic acid
-
50% inhibition at 0.0421 mM
2beta,3beta-2,3-dihydroxyolean-12-en-28-oic acid
-
-
3',4'-dihydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 5% inhibition of PTP-B1 at 0.02 mM
3,16-dioxo-olean-12(13),17(18)-diene
-
-
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-((5-[(N-acetyl-3-(4-[(carboxycarbonyl)(2-carboxyphenyl)amino]-1-naphthyl)-L-alanyl)amino]pentyl)oxy)-2-naphthoic acid
-
3-(1-carboxy-ethoxy)-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-(2,2'-dimethyl-carboxypropanoyloxy)-oleanolic acid
-
3-(2,5-dimethyl-1H-pyrrol-1-yl)-4-hydroxybenzoic acid
3-(2-carboxy-benzyloxy)-oleanolic acid
-
3-(2-carboxybenzoyloxy)-oleanolic acid
-
3-(3,5-dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonic acid (4-sulfamoylphenyl)-amide
-
3-(3,5-dibromo-4-hydroxy-benzoyl)-2-ethyl-benzofuran-6-sulfonicacid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.35 mM
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide
i.e. BBR
3-(3-carboxy-benzyloxy)-oleanolic acid
-
3-(4-carboxy-benzyloxy)-28-[4-butyric((s)-1-carboxyphenylethyl)-amide]-DELTA12-oleanene
-
3-(4-carboxy-benzyloxy)-oleanolic acid
-
3-(biphenyl-4-ylmethyl)-6-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
-
3-(carboxy-fluoro-methoxy)-6-chloro-benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-2-naphthoic acid
-
-
3-(carboxymethoxy)-5-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((1-(ethylsulfonyl)-piperidin-4-yl)amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(tetrahydro-2H-pyran-4-ylamino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-methylthieno(3,2-c)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)furo(2,3-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
-
reversible, competitive
3-(carboxymethoxy)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)thiophene-2-carboxylic acid
-
-
3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
-
3-benzyl-7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
3-benzyloxy-oleanolic acid
-
3-bromo-4-[(2,3-dibromo-4,5-dihydroxyphenyl)methyl]-5-(propoxymethyl)benzene-1,2-diol
86.15% inhibition at 0.02 mg/ml
3-bromo-4-[(2,3-dibromo-4,5-dihydroxyphenyl)methyl]-5-[(2-methylpropoxy)methyl]benzene-1,2-diol
96.25% inhibition at 0.02 mg/ml
3-bromo-4-[(2,3-dibromo-4,5-dihydroxyphenyl)methyl]-5-[[(propan-2-yl)oxy]methyl]benzene-1,2-diol
-
3-butyl-7-(2,4-dihydroxy-6-pentylphenoxy)-3,5-dimethoxy-2-benzofuran-1(3H)-one
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-carboxymethoxy-6-(4-hydroxyphenyl)-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-(5-methyl-1-phenyl-1H-pyrazol-3-ylcarbamoyl)-benzo(b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-phenylbenzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-thiophen-2-yl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-methyl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-naphtho(1,2-b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-thieno(3,2-c)quinoline-2-carboxylic acid
-
-
3-carboxypropanoyloxy-oleanolic acid
-
3-chlorobenzenecarboperoxoic acid
-
complete inhibition at 150 mM
3-dehydroxy-oleanolic acid
-
3-ethyl oxalyl-oleanolic acid
-
3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl 3-acetyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-hydroxy-4-(methoxycarbonyl)-5-methylphenyl 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoate
-
-
3-methyl-2-butenal
-
95% remaining activity at 0.5 mM
3-methylene-oleanolic acid
-
3-oxalyl-oleanolic acid
-
3-oxo-oleanolic acid
-
3-[(1-butyl-1,6-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-4-yl)oxy]-4,6-dihydroxy-2-pentylbenzoic acid
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
-
-
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
-
-
3-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
-
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
irreversible inhibition, detailed kinetic analysis of the interaction between E4 and the catalytic domain of enzyme STEP, overview. kinact is 0.068/s
3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
-
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
3-[oxalyl-amino]naphthalene-2-carboxylic acid
-
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,6-dicarboxylic acid
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
3alpha-angeloyloxypterokaurene L3
18% inhibition at 0.024 mM
3alpha-cinnamoyloxypterokaurene L3
-
3alpha-oleanolic acid
-
3alpha-tigloyloxypterokaurene L3
no inhibition at 0.024 mM
3beta,16a,17-trihydroxy-olean-12-ene
-
-
3beta-acetoxy-17beta-hydroxy-28-norolean-12-ene
-
-
3beta-acetoxy-28-hydroxyolean-12-ene
-
-
3beta-acetoxyolean-12-en-28-acid
-
-
3beta-acetoxyolean-12-en-28-aldehyde
-
-
3beta-hydroxyolean-12-en-28-oic acid
-
-
4'-carboxy-3'-hydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 10% inhibition of PTP-B1 at 0.02 mM
4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
-
4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
-
4,4'-methylenebis(3,5,6-tribromobenzene-1,2-diol)
78.64% inhibition at 0.02 mg/ml
4,4'-methylenebis(5,6-dibromobenzene-1,2-diol)
-
4,4'-[benzene-1,4-diylbis(methanediyloxy)]dibenzoic acid
-
4,6-bis(1,3,2-dithiarsolan-2-yl)-7-hydroxy-3H-phenoxazin-3-one
i.e. ReAsH
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid
-
50% inhibition at 39 nM for wild-type PTP-1B, at 39 nM for mutant V113I, at 45 nM for mutant M114V, at 29 nM for mutant V113I/M114V, at 32 nM for mutant G117E, at 142 nM for mutant L119V, and at 87 nM for isoform TCPTP wild-type and 24 nM for isoform TCPTP mutant V121L
4-((E)-2-nitrovinyl)benzoic acid
-
50% inhibition at 0.0027 mM in absence of 2-mercaptoethanol, at 0.425 mM in presence of 1 mM 2-mercaptoethanol
4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoic acid
4-(2,5-dimethyl-1H-pyrrol-1-yl)phthalic acid
4-(2-((5-(naphthalen-1-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoic acid
-
4-(2-((5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoic acid
-
4-(2-((6-chloro-5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoic acid
-
4-(3,5-dimethyl-1H-pyrazol-1-yl)aniline
DES-4799, enzyme binding structure, crystal structure analysis (PDB ID 8G65)
4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid
-
-
4-(3-ethyl-5-methyl-1H-pyrazol-1-yl)aniline
i.e. DES-5742, enzyme binding structure, crystal structure analysis (PDB ID 8G68)
4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
-
4-(5-ethyl-3-methyl-1H-pyrazol-1-yl)aniline
i.e. DES-5743, enzyme binding structure, crystal structure analysis (PDB ID 8G69)
4-(5-[5-(3,5-dichlorophenoxy)-2-furyl]-1,2,4-oxadiazol-3-yl)phenyl-N,N-dimethylsulfamate
85% inhibition at 0.2 mM
4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoic acid
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
dose-dependent increase in Y527 phosphorylation of Src
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5E)-5-[3-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-fluorobenzyl-1-cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
73% inhibition at 0.02 mg/ml
4-isoavenaciolide
potent irreversible inhibitor of VHR
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-(4-methoxyphenyl)isoxazole
-
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-phenylisoxazole
-
4-methyl-2-oxo-2H-1-benzopyran-7-yl ethenesulfonate
-
4-nitrophenyl phosphate
substrate inhibition at higher concentrations
4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-8-(phenylsulfanyl)-1,4-dihydro-1,7-naphthyridine-3-carboxylic acid
-
4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-[(1E)-3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-5-methoxy-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2,4-dihydroxy-6-pentadecylbenzoyl)oxy]-2-hydroxy-6-methylbenzoic acid
-
-
4-[(2,4-dihydroxy-6-propylbenzoyl)oxy]-2-hydroxy-6-propylbenzoic acid
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-bromobenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-tert-butylbenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl benzoate
-
-
4-[(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-(acetyloxy)-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(3-[(E)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
-
4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoic acid
-
-
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-[3-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-[4-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E)-3-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]prop-1-en-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy3, 70% inhibition at 250 nM AsCy3, AsCy3 is capable of specifically and potently inhibiting mutant enzyme asPTP1B in the presence of a complex proteome, while AsCy3 does not inhibit wild-type PTP1B activity in a cell lysate
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E,5E)-5-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]penta-1,3-dien-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy5
5-(2-fluoro-5-((1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]prop-1-en-1-yl)phenyl)isoxazole-3-carboxylic acid
-
5-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxybenzyl)thiazolidine-2,4-dione
67.90% inhibition at 0.02 mg/ml
5-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxybenzylidene)thiazolidine-2,4-dione
a potent protein tyrosine phosphatase 1B inhibitor with antidiabetic properties
-
5-(4-(3-bromo-2-(2,3-dibromo-4,5-dimethoxybenzyl)-4,5-dimethoxyphenoxy)benzyl)thiazolidine-2,4-dione
94.27% inhibition at 0.02 mg/ml
5-acetylamino-2-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
5-chloro-2-[methyl(methylidene)-lambda4-sulfanyl]-6-[(naphthalen-2-yl)oxy]-1H-benzimidazole
65% inhibition at 0.2 mM
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
mixed-type inhibition, complete inhibition at 0.2 mM
5-methoxy-4-[(1E)-3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6,8-difluoro-4-methyl-2-oxo-2H-1-benzopyran-7-yl ethenesulfonate
-
6-((1-(benzylsulfonyl)piperidin-4-yl)amino)-3-(carboxymethoxy)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM
6-(4-(3-(3-(benzyloxy)-2-(methoxycarbonyl)phenoxy)propyl)piperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 45.2 mg/ml
6-(4-benzylpiperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
62.3% inhibition at 0.02 mg/ml
6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-amino-1-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
12.4% inhibition at 0.02 mg/ml
6-benzyl-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
87.5% inhibition at 0.02 mg/ml
6-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-bromo-3-carboxymethoxy-benzo(b)-thiophene-2-carboxylic acid
-
-
6-bromo-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-chloro-7-(2,3-dihydro-1H-inden-1-ylamino)quinoline-5,8-dione
-
6-chloro-7-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-fluoro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
6-hydroxy-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]-1H-1,2,3-triazol-4-yl]-2-phenyl-1-benzofuran-5-carboxylic acid
-
-
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylate
-
80% residual activity at 0.1 mM
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
6-iodo-1-(4-methoxy-3-(methoxycarbonyl)benzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of more than 20 mg/ml
6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
-
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F
7-chloro-6-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
7-hydroxy-2-(1-(4-methoxybenzyl)-1H-imidazol-4-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-(4-methoxybenzyl)-1H-imidazol-5-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-pentyl-1H-imidazol-2-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-pentyl-1H-imidazol-4-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-pentyl-1H-imidazol-5-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-propyl-1H-imidazol-2-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-propyl-1H-imidazol-4-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1-propyl-1H-imidazol-5-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1H-imidazol-2-yl)-4H-chromen-4-one
-
7-hydroxy-2-(1H-imidazol-4-yl)-4H-chromen-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
7-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
7-hydroxy-2-(4-hydroxyphenyl)-3-[(3',4'-dihydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
60% inhibition of LMW-PTP isozyme 2, 25% inhibition of LMW-PTP 1, and 50% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenyl)-3-[(4'-carboxy-3'-hydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
5% inhibition of LMW-PTP isozyme 2, 10% inhibition of LMW-PTP 1, and 59% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
7-hydroxy-2-(4-hydroxyphenylpropyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
7-hydroxy-2-[1-[(4-methoxyphenyl)methyl]-1H-imidazol-2-yl]-4H-1-benzopyran-4-one
-
8-(2-[4-[(E)-2-carboxyethenyl]phenyl]-1,3-thiazol-4-yl)dibenzo[b,d]furan-4-carboxylic acid
-
8-acetyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
8-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylic acid
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
abietic acid
a nonpolar inhibitor and weak mixed-type inhibitor of PTP1B, inhibits the enzyme by binding to its active site in a nonsubstrate-like manner that stabilizes the catalytically essential WPD loop in an inactive conformation, modelling of enzyme binding. Upon binding to the active site, abietic acid forms a hydrogen bond with R221 that weakens a bond between R221 and E115 and prevents the formation of a hydrogen bond between W179 and R221 that forms when the WPD loop closes
acanthoic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.024 mM
acetaldehyde
-
more than 95% remaining activity at 0.5 mM
acid
-
-
-
acrolein
-
4% remaining activity at 0.5 mM, potent irreversible time-dependent inhibitor, addition of 1 mM vanadate slows inactivation of PTP1B by 0.5 mM acrolein
aquastatin A
-
derived from marine fungus Cosmospora sp. SF-5060, competitive inhibition
auranofin
-
inhibition of cysteine-dependent protein tyrosine phosphatases
benzenesulfonyl fluoride
-
Benzonitrile
-
benzyl 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
0.1% inhibition at 0.02 mg/ml
benzyl 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
80.5% inhibition at 0.02 mg/ml
benzyl oleanolic acid amide
-
benzyl oleanolic acid ester
-
Berberine
binding structure, molecular modeling, overview
betulinic acid
-
95.1% PTP1B inhibitory activity with 0.0007 mg/ml
betulinic acid methyl ester
-
89.4% PTP1B inhibitory activity with 0.00093 mg/ml
biphenyl-3,4-diol
25% inhibition of LMW-PTP isozyme 2, and 10% inhibition of LMW-PTP 1 and PTP-B1 at 0.02 mM
bis(2,3,6-tribromo-4,5-dihydroxyphenyl)methanone
complete inhibition at 0.02 mg/ml
bis(2-ethyl-maltolato)oxidovanadium(IV)
noncompetitive inhibition of hydrolysis of 4-nitrophenyl phosphate and of phosphorylated undecapeptide substrate EGFR988-998 in the presence of bis(2-ethyl-maltolato)oxidovanadium(IV)
bis(2-methyl-maltolato)oxidovanadium(IV)
-
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
-
bis(acetylacetonato)oxidovanadium(IV)
acts as an uncompetitive inhibitor of PTP1B with DADEpYLIPQQG as the substrate, but this VO2+-chelate exhibits only apparent competitive inhibition of 4-nitrophenyl phosphate hydrolysis when catalyzed by PTP1B, differing from that observed in the hydrolysis of the phosphotyrosine-containing undecapeptide DADEpYLIPQQG mimicking residues 988-998 of the epidermal growth factor receptor (EGFR). Addition of 4-nitrophenyl phosphate after addition of saturating amounts of bis(acetylacetonato)oxidovanadium(IV) to PTP1B causes complete loss of catalytic activity
BzN-EJJ-amide
calopocarpin
-
-
chloro(1,3-dimethyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(p-MeMeIm)AuICl]
chloro(1-methyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(MeIm)AuICl]
chloro[1-methyl-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazol-2-yl]gold
-
i.e. [(p-MeBzMeIm)AuICl]
CinnGel 2ME
continentalic acid
corosolic acid
-
50% inhibition at 0.0072mM, mixed-type inhibition
Cr(VI)
-
as Na2CrO4, induces clonogenic lethality
crotonaldehyde
-
85% remaining activity at 0.5 mM
cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
71.1% inhibition at 0.02 mg/ml
dehydroabietic acid
dehydrocostuslactone
-
86.2% PTP1B inhibitory activity with 0.00651 mg/ml
dihydroabietic acid
diphosphate
-
-
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.010 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0096 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
dysidiolide
inhibits Cdc25A
ent-17-hydroxykaur-15-en-19-oic acid
40% inhibition at 0.033 mM
ent-3beta-angeloyloxykaur-16-en-19-oic acid
-
ent-3beta-tigloyloxykaur-16-en-19-oic acid
-
ent-kaur-16-en-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.020 mM
ent-kaur-9(11),16-dien-19-oic acid
29% inhibition at 0.033 mM
ertiprotafib
-
erybraedin A
-
-
erylysins A
-
i.e. 3''-hydroxy-2',2'-dimethylpyrano[6',5':3,4]-2'',2''-dimethyldihydropyrano[6'',5'':9,10]pterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
erylysins B
-
i.e. furano[5',4':3,4]-9-hydroxy-10-prenylpterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
erysubin D
-
-
eryvarin D
-
-
ethyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoate
-
-
ethyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoate
-
-
ethyl (4R)-4-[(E)-2-(4-bromophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-(4-chlorophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-(4-fluorophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-(4-methoxyphenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-(4-methylphenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-(4-nitrophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-4-[(E)-2-phenylethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl (4R)-6-(propan-2-yl)-2-sulfanylidene-4-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 2-(2-((5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)thiazole-4-carboxylate
-
ethyl 2-(2-bromophenyl)-4-[(4-methoxyphenoxy)methyl]-1,3-thiazole-5-carboxylate
reaction mode analysis by molecular docking and molecular dynamics simulation
ethyl 2-(2-bromophenyl)-4-[(4-methylphenoxy)methyl]-1,3-thiazole-5-carboxylate
-
ethyl 2-(2-bromophenyl)-4-[(4-nitrophenoxy)methyl]-1,3-thiazole-5-carboxylate
-
ethyl 2-(4-bromophenyl)-4-[(4-methoxyphenoxy)methyl]-1,3-thiazole-5-carboxylate
-
ethyl 2-(4-bromophenyl)-4-[(4-nitrophenoxy)methyl]-1,3-thiazole-5-carboxylate
-
ethyl 2-(4-fluorophenyl)-4-[(4-methylphenoxy)methyl]-1,3-thiazole-5-carboxylate
-
ethyl 4-(2-((5-(naphthalen-1-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoate
-
ethyl 4-(2-((5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)acetamido)benzoate
-
ethyl 4-[(4-chlorophenoxy)methyl]-2-(3-phenoxyphenyl)-1,3-thiazole-5-carboxylate
-
ethyl 4-[(4-methoxyphenoxy)methyl]-2-(3-nitrophenyl)-1,3-thiazole-5-carboxylate
-
ethyl 4-[(4-methylphenoxy)methyl]-2-(3-nitrophenyl)-1,3-thiazole-5-carboxylate
-
ethyl 4-[(4-methylphenoxy)methyl]-2-(3-phenoxyphenyl)-1,3-thiazole-5-carboxylate
-
ethyl 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoate
-
-
ethyl [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetate
-
-
ethyl-3,4-dephostatin
-
FlAsH
the small molecule biarsenical fluorescein derivative, FlAsH, is no inhibitor of the wild-type enzyme but of the engineered WPD insertion mutant enzyme that displays FlAsH-binding cysteine residues. Inhibition of the FlAsH-sensitized TCPTP mutants is rapid and specific, and strong FlAsH sensitivity is observed in mutants that contain as few as two cysteine point mutations in their engineered WPD loops, minimization of FlAsH-binding determinants, overview
fluorescein arsenical hairpin binder
fluorescein arsenical hairpin binder does not inhibit any wild type PTP, but insertion of a fluorescein arsenical hairpin binder-binding peptide (CCPGCC) at a conserved position in the PTP catalytic-domain's WPD loop confers fluorescein arsenical hairpin binder sensitivity upon divergent PTPs
-
glycyrrhetic acid
-
-
Glyoxal
-
93% remaining activity at 0.5 mM
glyoxalbis(N(4)-methylthiosemicarbazonato)Cu(II)
-
inhibition of protein tyrosine phosphatase activity is the prerequisite for activation of epidermal growth factor receptor by the compound, overview
H3VO4
heparin
hesperetin
uncompetitive inhibition
hesperetin 5-O-glucoside
mixed-type inhibition
-
hesperetin 7-O-glucoside
low inhibition
hesperidin
mixed-type inhibition. The hesperidin sugar moieties form hydrogen bond interactions with the Glu115, Lys120, Arg221, Phe182, Pro180, Gln266, and Gly183 residues of PTP1B, and the interacting methoxy group forms single alkyl bond interactions with Ala17
hexadecanoyl-5-hydroxymethyl tetronic acid
potent irreversible inhibitor of VHR
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.005 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0023 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0037 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0021 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0016 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.007 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00049 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
isoneorautenol
-
-
isopimaric acid
isothiocyanatobenzene
-
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview
L-Tartrate
-
weak
licochalcone A
-
licochalcone E
-
lithocholic acid
-
natural inhibitor against PTP1B
lobaric acid
-
a depsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
lupenone
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
lupeol
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
maslinic acid
menadione
inhibits Cdc25B irreversibly
methyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoate
-
-
methyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoate
-
-
methyl (4R)-4-[(E)-2-(4-bromophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-4-[(E)-2-(4-bromophenyl)ethenyl]-6-tert-butyl-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-4-[(E)-2-(4-chlorophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
methyl (4R)-4-[(E)-2-(4-fluorophenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
methyl (4R)-4-[(E)-2-(4-methoxyphenyl)ethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-4-[(E)-2-phenylethenyl]-6-(propan-2-yl)-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-(propan-2-yl)-2-sulfanylidene-4-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-2-sulfanylidene-4-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-(4-chlorophenyl)ethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-(4-fluorophenyl)ethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-(4-methoxyphenyl)ethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-(4-methylphenyl)ethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-(4-nitrophenyl)ethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl (4R)-6-tert-butyl-4-[(E)-2-phenylethenyl]-2-sulfanylidene-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 2-(3-(1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 6.5 mg/ml
methyl 2-(3-(1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 9.4 mg/ml
methyl 2-[4-[(4-[[ethoxy(oxo)acetyl][2-(methoxycarbonyl)phenyl]amino]-3-ethylphenylalanyl)amino]butoxy]-6-hydroxybenzoate
-
methyl 3,8-dimethoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 3-formyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 4,4-dimethyl-3-oxochol-5-en-24-oate
-
-
methyl 5-amino-6-(7-amino-6-methoxy-5,8-dioxo-5,8-dihydroquinolin-2-yl)-4-(2-hydroxy-3,4-dimethoxyphenyl)-3-methylpyridine-2-carboxylate
-
methyl 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl oleanolic acid amide
-
methyl oleanolic acid ester
-
methyl phenylcarbamate
-
methyl-5-((3-(benzylcarbamoyl)-6-iodo-4-oxoquinolin-1(4H)-yl)methyl)-2-methoxybenzoate
-
IC50 of more than 20 mg/ml
mokko lactone
-
93.1% PTP1B inhibitory activity with 0.00141 mg/ml
molybdate
mpV(pic)
-
potent and selective PTP inhibitor, inhibits SPH-1 in a dose-dependent manner
MSI-1436
small molecule inhibitor MSI-1436 binds to the disordered C-terminal domain of PTP1B, C-terminal to the catalytic domain, MSI-1436 functions using an allosteric mechanism to direct the enzymatic activity of PTP1B
N,1-dibenzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
41.4% inhibition at 0.02 mg/ml
N,1-dibenzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
61.8% inhibition at 0.02 mg/ml
N,N'-[benzene-1,4-diylbis(propane-2,2-diylbenzene-4,1-diyl)]bis(1,1,1-trifluoromethanesulfonamide)
-
-
N-((4-((E)-2-nitroethenyl)phenyl)carbonyl)glycyl-L-alpha-glutamyl-L-glutamic acid
-
50% inhibition at 0.0014 mM in absence of 2-mercaptoethanol, at 0.275 mM in presence of 1 mM 2-mercaptoethanol
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
inhibition of enzyme increases caveolin-1 phosphorylation
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
N-(1,3-benzothiazol-2-yl)-2-chloroacetamide
modeling of PTP1B bound to the compound
N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-(4-methylphenyl)acetamide
-
N-(3-chloro-4-fluorophenyl)-2-[(6,7-dimethoxy-4-oxo-3-phenyl-3,4-dihydro-2-quinazolinyl)sulfanyl]acetamide
80% inhibition at 0.2 mM
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
N-(3-methylisoxazol-5-yl)-2-((5-(naphthalen-2-yloxy)-1H-benzimidazol-2-yl)thio)acetamide
-
N-(3-[(3,5-difluorobenzyl)oxy]pyridin-2-yl)-4-pentylbenzenesulfonamide
74% inhibition at 0.2 mM
N-(3-[(4-chlorophenyl)sulfanyl]-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide
-
N-([1,1'-biphenyl]-3-yl)-2-chloroacetamide
-
N-([4-[difluoro(phosphono)methyl]phenyl]acetyl)-a-aspartyl-4-[difluoro(phosphono)methyl]phenylalaninamide
-
-
N-1-(2-[(2-oxo-4-propyl-2H-chromen-7-yl)oxy]propanoyl)-3-(trifluoromethyl)benzene-1-sulfonohydrazide
84% inhibition at 0.2 mM
N-benzoyl-L-glutamyl-[4-phosphono(difluoromethyl)]-L-phenylalanineamide
-
i.e. BzN-EJJ-amide, 50% inhibition at 4 nM
N-benzyl-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
N-benzyl-1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
6.1% inhibition at 0.02 mg/ml
N-benzyl-2-chloroacetamide
-
N-phenylethenesulfonamide
-
N-phenylprop-2-enamide
-
N-[1-(1H-benzimidazol-2-yl)-2-[3-methyl-4-(1,1,3-trioxo-1lambda6,2-thiazolidin-5-yl)phenyl]ethyl]benzenesulfonamide
-
N-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl]-4-tert-butylbenzamide
-
-
N-[5-(dimethylamino)-2-hydroxy-3-methoxybenzyl]-N-methyl-2-(4-nitrophenyl)ethanaminium
-
N-[6-chloro-5-(2,3-dichlorophenoxy)-1-methyl-1H-benzimidazol-2-yl]acetamide
70% inhibition at 0.2 mM
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
mixed-type inhibition, 92% inhibition at 0.2 mM
N2-(2-((2-((N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalanyl)amino)ethyl)disulfanyl)ethyl)-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-argininamide
-
in presence of 5-50 nM, 11-35% decrease in cell spreading, 24% decrease in number of migratory cells, dose-dependent increase in Y527 phosphorylation of Src
Na3VO4
-
-
naphthalen-2-yl ethenesulfonate
-
NAT6-297775
-
-
neohesperidin
uncompetitive inhibition
NO
-
inactivation, phosphate protects
nocardione A
inhibits Cdc25B
nocardione B
inhibits Cdc25B
NSC-87877
-
potent Shp2 and Shp1 inhibitor
oleanolic acid
oleanolic acid amide
-
oleanolic alcohol
-
oleanonic acid
-
-
orientanol C
-
-
orthovanadate
papaverine
binding structure, molecular modeling, overview
paracaseolide A
-
-
peracetic acid
-
a potent, time-dependent inactivator of the catalytic subunit of PTP1B, treatment of the enzyme with 0.015 mM for 15 sec inactivates 88% of the enzyme, inactivation of PTP1B by peracetic acid can be reversed by treatment of the enzyme with thiols
phaseollin
-
-
phenyl bromoacetate
-
phenyl prop-2-enoate
-
phenyl vinyl sulfone
PVS, the compound is cell-permeable, owing to its relatively simple structure and lack of charged functional groups
phenyl vinylsulfonate
PVSN, the compound is cell-permeable, owing to its relatively simple structure and lack of charged functional groups
Phenylarsine oxide
phenylhydrazonopyrazolone sulfonate 1
-
potent, active site-directed small molecule inhibitor which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B
phenylhydrazonopyrazolone sulfonate 4
-
the most potent inhibitor of Shp2 which shows a specificity profile similar to phenylhydrazonopyrazolone sulfonate 1
phosphate
PO43-
-
treatment of the enzyme with 0.05 mM PO43- for 15 sec inactivates 49% of the enzyme
poly(Glu-Tyr)
-
-
pomolic acid
-
-
potassium bisperoxo(1,10-phenanthroline)oxovanadate
propanal
-
93% remaining activity at 0.5 mM
pterokaurene L3
no inhibition at 0.031 mM
rilobolide-6-O-methacrylate
no inhibition at 0.026 mM
RK-682
rotungenic acid
-
-
small t antigen
-
small t antigen of DNA tumor virus SV40 inhibits the phosphatase activity of the PP2A core enzyme
-
sodium orthovanadate
sodium pervanadate
-
broad-acting tyrosine phosphatase inhibitor
Sodium vanadate
spathodic acid
-
-
spermidine
-
-
spermine
-
2.0-20 mM
stevastelin
inhibits VHR
stigmasterol
-
-
sulfircin
inhibits Cdc25A
suramin
taraxerol
-
-
tetrachyrin
-
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00025 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.08 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
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suramin-derivative, 50% inhibition of PTP1B at 0.0045 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
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suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
trilobolide-6-O-isobutyrate
no inhibition at 0.026 mM
trodusquemine
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tungstate
ursolic acid
uvaol
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vanadate
VO3N3
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oxovanadium(IV) is coordinated with one nitrogen and two oxygen atoms from the Schiff base and two nitrogen atoms from the bidentate planar ligands, in a distorted octahedral geometry, VO3N3
wedelolide D
32% inhibition at 0.020 mM
wedelolide H
no inhibition at 0.023 mM
wedelolide I
no inhibition at 0.021 mM
wedelolide J
no inhibition at 0.021 mM
ZINC39276654
used as scaffold for inhibitor design
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[(4-[(4E)-2-(1H-benzotriazol-1-yl)-2-[4-(methoxycarbonyl)phenyl]-5-phenylpent-4-en-1-yl]phenyl)(difluoro)methyl]phosphonic acid
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[(E)-2-nitroethenyl]benzene
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[1,1'-biphenyl]-3-yl ethenesulfonate
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[2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid
irreversible inhibition
[3-bromo-2-[(2,3-dibromo-4,5-dimethoxyphenyl)methyl]-4,5-dimethoxyphenyl]methanol
74.86% inhibition at 0.02 mg/ml
[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetic acid
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[7-[4-[2-(1H-benzotriazol-1-yl)-2-[4-[difluoro(phosphono)methyl]phenyl]-3-phenylpropyl]phenyl]-2-(1-methoxy-3-methylbutyl)quinolin-8-yl]phosphonic acid
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[[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid
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[[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
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additional information
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,2-epoxy-3-(p-nitrophenoxy)propane
C215D mutant, not wild type
2,3-diphosphoglycerate
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activation
2-mercaptoethanol
-
activation
2-mercaptoethylamine
-
activation
ADP
-
activation
dithiothreitol
-
activation
DTT
activates
EDTA
-
activation
glutathione
-
activation
IGF-I
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IGF-I stimulates p52shc phosphorylation, with a significantly greater increase in p52shc phosphorylation in the p66shc knockdown cells compared to control cells. Overexpression of p66shc impairs IGF-I-stimulated p52shc tyrosine phosphorylation
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NaCl
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activity against phosphotyrosine, optimal at 0.1 M
phorbol 12-myristate 13-acetate
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enzyme gene is among the 10 genes with the largest increased in expression upon phorbol 12-myristate 13-acetate stimulation
spermidine
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activation
spermine
sulfhydryl compounds
-
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suramin
-
0.01 mM, about 30% increase in activity of isoforms PTPalpha, LAR
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
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0.01 mM, up to 4.5 activation of isoform PTPalpha wild-type
Triton X-100
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0.1%, 25-30% activation
UpA
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uPA regulates SHP-2 phosphorylation, stimulates its catalytic activity and association with PDGFR-beta and with lipid rafts
additional information
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