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Literature summary for 3.1.3.48 extracted from

  • Fukuda, S.; Ohta, T.; Sakata, S.; Morinaga, H.; Ito, M.; Nakagawa, Y.; Tanaka, M.; Matsushita, M.
    Pharmacological profiles of a novel protein tyrosine phosphatase 1B inhibitor, JTT-551 (2010), Diabetes Obes. Metab., 12, 299-306.
    View publication on PubMed

Application

Application Comment Organism
medicine the PTPB1 inhibitor JTT-551 improves glucose metabolism by enhancement of insulin signalling and can be useful in the treatment of type 2 diabetes mellitus Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
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 Homo sapiens
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. The inhibitor shows a hypoglycaemic effect in ob/ob mice, overview Mus musculus
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. The inhibitor shows a hypoglycaemic effect in rat L6 cells, overview Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
C57BL/6J mice and male ob/ob mice
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation purified recombinant enzyme Homo sapiens
-
L-6 myoblast cell a skeletal myoblast cell line Rattus norvegicus
-
T-lymphocyte
-
Mus musculus
-
T-lymphocyte
-
Homo sapiens
-
T-lymphocyte
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-nitrophenyl phosphate + H2O
-
Mus musculus 4-nitrophenol + phosphate
-
?
4-nitrophenyl phosphate + H2O
-
Homo sapiens 4-nitrophenol + phosphate
-
?
4-nitrophenyl phosphate + H2O
-
Rattus norvegicus 4-nitrophenol + phosphate
-
?

Synonyms

Synonyms Comment Organism
CD45 protein tyrosine phosphatase
-
Mus musculus
CD45 protein tyrosine phosphatase
-
Homo sapiens
CD45 protein tyrosine phosphatase
-
Rattus norvegicus
LAR
-
Mus musculus
LAR
-
Homo sapiens
LAR
-
Rattus norvegicus
leucocyte common antigen-related protein tyrosine phosphatase
-
Mus musculus
leucocyte common antigen-related protein tyrosine phosphatase
-
Homo sapiens
leucocyte common antigen-related protein tyrosine phosphatase
-
Rattus norvegicus
protein tyrosine phosphatase 1B
-
Mus musculus
protein tyrosine phosphatase 1B
-
Homo sapiens
protein tyrosine phosphatase 1B
-
Rattus norvegicus
PTP1B
-
Mus musculus
PTP1B
-
Homo sapiens
PTP1B
-
Rattus norvegicus
T-cell protein tyrosine phosphatase
-
Mus musculus
T-cell protein tyrosine phosphatase
-
Homo sapiens
T-cell protein tyrosine phosphatase
-
Rattus norvegicus
TCPTP
-
Mus musculus
TCPTP
-
Homo sapiens
TCPTP
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00022
-
JTT-551 pH 7.5, 22°C, PTPB1 Rattus norvegicus
0.0093
-
JTT-551 pH 7.5, 22°C, TCPTP Rattus norvegicus
0.03
-
JTT-551 above, pH 7.5, 22°C, CD45 and LAR Rattus norvegicus