Properties of the kinase and phosphatase inhibitors and NaAsO2
Enzyme | Agent | EC50 | Conc. Useda | Mechanism | References | |
|---|---|---|---|---|---|---|
| μM | ||||||
| p38 | SB 203580 | 0.6 | 30 | Competitive binding in the ATP pocket | Woo et al. (2005) | |
| SKF 86002 | 1 | 30 | Competitive binding in the ATP pocket | Prabhakar et al. (1993); Pelaia et al. (2005) | ||
| JNK | SP 600125 | 0.19 | 30 | Competes with ATP to inhibit the enzyme | Woo et al. (2005) | |
| Dicumarol | 5 | 15 | Blocks stress signaling by the inhibition of quinone reductase | Cross et al. (1999) | ||
| ERK | PD 98059 | 2 | 50 | Inhibits activation of ERK by blocking upstream enzyme mitogen-activated protein kinase kinase | English and Cobb (2002); Woo et al. (2005) | |
| U 0126 | 0.5 | 30 | Inhibits activation of ERK by blocking upstream enzyme mitogen-activated protein kinase kinase | English and Cobb (2002); Hirst et al. (2002) | ||
| PKC | Chelerythrine | 0.66 | 20 | Competitive binding to the phosphate acceptor of the enzyme | Herbert et al. (1990) | |
| PI-3-K | LY 294002 | 1.4 | 50 | Blocks the ATP-binding site of the enzyme | Vlahos et al. (1994) | |
| CaM-K-II | KN-62 | 1 | 20 | Binds directly to the calmodulin binding site of the enzyme | Tokumitsu et al. (1990); Massé and Kelly (1997) | |
| MLCK | ML-7 | 0.3 | 30 | Inhibits the binding of ATP to MLCK | Shen et al. (2002); Göggel and Uhlig (2005) | |
| Phosphatase | Na3VO4 | 30-50 | 300 | Analog to phosphate intermediates | Gordon (1991); Pugazhenthi et al. (1996) | |
| Stress-activated protein kinases | NaAsO2 | 60 | 300 | Stress inducer (activates stress-sensitive protein kinases) | Ludwig et al. (1998); Flatman and Creanor (1999) | |
↵ a Concentrations (Conc.) commonly reported in literature were used in this study.