Table 1.
Summary Comparison of AMPK Isoform Properties. n.d. = Not Determined, n.a. = Not Applicable
| ATP Km (µM) | Inhibitor | |||||||
|---|---|---|---|---|---|---|---|---|
| AMPK Isoform | Assay Format | - AMP | + AMP (100 µM) | IC50(nM) | Activator EC50(µM) / Max. fold-activation | |||
| Cpd C | AMP | ZMP | APR | ATMP | ||||
| α1β1γ1 | Radiometric | 34 | 74 | 230 | 1.6 / 1.7-fold | 165 / 1.5-fold | n.d. / n.a. | 0.7 / 1.7-fold |
| α1β1γ1 | TR-FRET | n.d. | n.d. | 700 | 1.4 / n.a. | 74 / n.a. | 722 / n.a. | 0.25 / n.a. |
| α1β1γ1 | FRET | 35 | 83 | 320 | 2.5 / 2.8-fold | 112 / 3.3-fold | n.d. / n.a. | 0.35 / 3.3-fold |
| α1β1γ1 | CHEF | 31 | 25 | 343 | 0.6 / 1.8-fold | 36 / 1.8-fold | n.d. / n.a. | 0.25 / 1.8-fold |
| α2β1γ1 | Radiometric | 65 | 73 | 88 | 1.4 / 2.5-fold | 54 / 2.5-fold | 194 / 1.9-fold | 0.13 / 2.9-fold |
| α2β1γ1 | TR-FRET | n.d. | n.d. | 500 | 0.35 / n.a. | 23 / n.a. | 43 / n.a. | 0.04 / n.a. |
| α2β1γ1 | FRET | 165 | 154 | 140 | 1.4 / 5-fold | 40 / 6.3-fold | n.d. / n.a. | 0.10 / 6.3-fold |
| α2β1γ1 | CHEF | 82 | 55 | 184 | 0.23 / 2.5-fold | 40 / 2.2-fold | n.d. / n.a. | 0.07 / 2.5-fold |