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Literature summary for 3.1.3.48 extracted from

  • Na, M.; Kim, B.Y.; Osada, H.; Ahn, J.S.
    Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta (2009), J. Enzyme Inhib. Med. Chem., 24, 1056-1059.
    View publication on PubMed

Application

Application Comment Organism
drug development PTP1B is a target for drug development in treatment of type II diabetes and obesity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
lupenone isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner Homo sapiens
lupeol isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner Homo sapiens
RK-682
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant PTPB1 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
protein tyrosine phosphatase 1B
-
Homo sapiens
PTP1B
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Homo sapiens
0.0034
-
lupeol pH 6.0, 37°C Homo sapiens
0.0118
-
lupenone pH 6.0, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0045
-
pH 6.0, 37°C Homo sapiens RK-682
0.0056
-
pH 6.0, 37°C Homo sapiens lupeol
0.0137
-
pH 6.0, 37°C Homo sapiens lupenone