EC Number   |
Inhibitors |
Structure |
|---|
   2.3.1.85 | (+)-catechin |
50% inhibition of overall enzyme reaction at 1.6 mM, 50% inhibition of ketoacyl reduction reaction at 7.4 mM |
   |
| 2.3.1.85 | (+-)-taxifolin |
50% inhibition at 0.041163 mM |
|
| 2.3.1.85 | (-)-catechin gallate |
50% inhibition at 0.0015 mg/ml, B ring, C ring and gallate ring of inhibitor react with acyl transferase domain |
|
| 2.3.1.85 | (-)-epicatechin |
50% inhibition of overall enzyme reaction at 3.8 mM, 50% inhibition of ketoacyl reduction reaction at 9.38 mM |
|
| 2.3.1.85 | (-)-epicatechin gallate |
50% inhibition of overall enzyme reaction at 0.042 mM, 50% inhibition of ketoacyl reduction reaction at 0.068 mM, two-step inhibition mechanism with reversible initial inhibition and irreversible subsequent inactivation |
|
| 2.3.1.85 | (-)-epigallocatechin gallate |
0.5 mM, 20% residual activity, 50% inhibition of overall enzyme reaction at 0.052 mM, 50% inhibition of ketoacyl reduction reaction at 0.1 mM |
|
| 2.3.1.85 | (10E,12Z)-octadec-10,12-dienoic acid |
more potent inhibitor than (9Z,11E)-octadec-9,11-dienoic acid |
|
| 2.3.1.85 | (9Z,11E)-octadec-9,11-dienoic acid |
- |
|
| 2.3.1.85 | 1,1'-[methanediylbis(2,4,6-trihydroxy-5-methylbenzene-3,1-diyl)]dibutan-1-one |
IC50: 0.0254 mM |
|
| 2.3.1.85 | 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 |
|
