Table 1.
Platensimycin is a highly selective mammalian FAS inhibitor
| Platensimycin | Platencin | C75 | TOFA | Cerulenin | |
| Purified enzyme | |||||
| Human FAS (IC50, μM) | 0.3 | 6.3 | >100 | >100 | ND |
| Rat FAS (IC50, μM) | 0.2 | 2.5 | >100 | >100 | ND |
| Rat hepatocytes | |||||
| Fatty acid synthesis (IC50, μM) | 0.1 | 2.0 | 13 | 0.4 | 86.7 |
| Sterol synthesis (IC50, μM) | >>100 | >>100 | 6.6 | 9.3 | 101.6 |
| Selectivity (FA/sterol) | >>1075 | >>50 | 0.6 | 13.4 | 1.0 |
| Fatty acid oxidation (% of control) | 59.7 at 10 μM | 66 at 10 μM | 156 at 40 μM | 245 at 10 μM | 81 at 40 μM |
| LDH assay (% of cell death) | 0 at 100 μM | 0 at 100 μM | 13.3 at 40 μM | 0 at 100 μM | 8.5 at 40 μM |
IC50 values are the average of triplicate determinations, except for the IC50 of platencin for rat FAS, which was n = 1. All IC50 values in the FAS assay were obtained without preincubation with the inhibitors. ND, not determined.