TABLE 1

Summary of the pharmacology, potency, and source of inhibitors




Pharmacology

Approximate Potencya

Source
U73122 Phospholipase C inhibitor IC50 = 1.0–2.1b Tocris Cookson Inc., Ellisville, MO
GF109203X Protein kinase C IC50 = 0.0084–5.8b Tocris Cookson Inc.
1-Butanol Phospholipase D inhibitor IC50 = 10,000 Sigma-Aldrich
CGP77675 c-Src inhibitor IC50 = 0.04 Novartis, Basel, Switzerland
HA1077 Rho kinase inhibitor Ki = 0.4 Calbiochem, San Diego, CA
Y27632 Rho kinase inhibitor Ki = 0.14 Tocris Cookson Inc.
LY294002 Phosphatidylinositol-3-kinase inhibitor IC50 = 1.4 Tocris Cookson Inc.
Dipenylene-iodonium NADPH oxidase inhibitor IC50 = 0.3 Sigma-Aldrich
Tempol Superoxide dismutase mimetic EC50 = 54–436c Sigma-Aldrich
C2-Ceramide Phospholipase D inhibitor IC50 = 5 Tocris Cookson Inc.
PP1
Src inhibitor
IC50 = 0.005–0.17b
Tocris Cookson Inc.
  • a , Concentrations are in micromoles per liter

  • b , Potency differs according to specific isoform/family member of enzyme

  • c , Potency is highly dependent on assay system