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Literature summary for 2.7.1.137 extracted from

  • El-Kholy, W.; Macdonald, P.E.; Lin, J.H.; Wang, J.; Fox, J.M.; Light, P.E.; Wang, Q.; Tsushima, R.G.; Wheeler, M.B.
    The phosphatidylinositol 3-kinase inhibitor LY294002 potently blocks K(V) currents via a direct mechanism (2003), FASEB J., 17, 720-722.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
additional information insulin stimulates Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
LY294002 the inhibitor potently, reversibly blocks voltage-dependent K+ channel currents via a direct mechanism, IC50 is 0.009 mM, potentiates glucose-stimulated insulin secretion from MIN6 cells in vivo Rattus norvegicus
LY303511 the inhibitor potently, reversibly blocks voltage-dependent K+ channel currents via a direct mechanism, IC50 is 0.065 mM Rattus norvegicus
additional information no inhibition by 5,6-dichlorobenzimidazole Rattus norvegicus
Wortmannin specific inhibition, no blockage of whole-cell outward K+ currents Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ as MgATP2- Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
insulinoma cell
-
Rattus norvegicus
-
MIN-6 cell insulinoma cell Mus musculus
-
pancreatic beta cell
-
Rattus norvegicus
-
pancreatic islet
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
phosphatidylinositol 3-kinase
-
Rattus norvegicus
PI3K
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.2 7.3 assay at Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP as MgATP2- Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.009
-
the inhibitor potently, reversibly blocks voltage-dependent K+ channel currents via a direct mechanism, IC50 is 0.009 mM, potentiates glucose-stimulated insulin secretion from MIN6 cells in vivo Rattus norvegicus LY294002
0.065
-
the inhibitor potently, reversibly blocks voltage-dependent K+ channel currents via a direct mechanism, IC50 is 0.065 mM Rattus norvegicus LY303511