EC Number   |
Inhibitors |
Structure |
|---|
    1.1.1.100 | (E)-1-(4-methylpiperidin-1-yl)-3-phenylprop-2-en-1-one |
80% residual activity |
   |
| 1.1.1.100 | (E)-2-nitrophenyl cinnamate |
- |
|
| 1.1.1.100 | (E)-3-phenoxybenzyl 3-(benzo[d][1,3]dioxol-5-yl)acrylate |
61% residual activity |
|
| 1.1.1.100 | (E)-4-cyanophenyl 3-(benzo[d][1,3]dioxol-5-yl)acrylate |
- |
|
| 1.1.1.100 | (E)-benzyl 3-(benzo[d][1,3]dioxol-5-yl)acrylate |
71% residual activity |
|
| 1.1.1.100 | (E)-phenyl 3-(benzo[d][1,3]dioxol-5-yl)acrylate |
69% residual activity |
|
| 1.1.1.100 | 1,2,3,4,6-penta-O-galloyl-beta-D-glucose |
mixed type of inhibition. IC50 value 0.9 microgramm per ml, Ki value 0.21 microgramm per ml |
|
| 1.1.1.100 | 1,2,3,4,6-penta-O-galloyl-beta-D-glucose |
minimal inhibitory concentration 0.125 mg/ml |
|
| 1.1.1.100 | 1,2,3,4,6-penta-O-galloyl-beta-D-glucose |
minimal inhibitory concentration 0.25 mg/ml |
|
| 1.1.1.100 | 1,2,3,4,6-penta-O-galloyl-beta-D-glucose |
compound is transported across cancer cell membrane to further down-regulate FAS and activate caspase-3 in MDA-MB-231 cells. Compared with other FAS inhibitors, including catechin gallate and morin, 1,2,3,4,6-penta-O-galloyl-beta-D-glucose involves a higher reversible fast-binding inhibition with an irreversible slow-binding inhibition, i.e. saturation kinetics with a dissociation constant of 0.59 microM and a limiting rate constant of 0.16 per min. The major reacting site of PGG is on the beta-ketoacyl reduction domain of FAS. Compound exhibits different types of inhibitions against the three substrates in the FAS overall reaction |
|
