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 |