Table 1.
Analysis of Sfp-type PPTase standard inhibitors
| IC50 (μM) - VibB | ||
|---|---|---|
| Compound | Sfp | hPPTase |
| 2′-deoxy-3,5-phosphoadenosine | 11 ± 1 | 51 ± 1 |
| 3,5-phosphoadenosine | 7 ± 1 | 6 ± 1 |
| coenzyme A | 8 ± 1 | 14 ± 1 |
| Mitoxantrone 2HC1 | Inactive | Inactive |
| benserazide HCl | Inactive | NC |
| Bay 11-7085 | Activator | Inactive |
| SCH-202676 HBr | 0.2 ± 1 | NC |
| 6-nitroso-1,2-benzopyrone | 3 ± 1 | Inactive |
| PD 404,182 | 1 ± 1 | Inactive |
| guanidinyl-naltrindole ditrifluoroacetate | Activator | NC |
| sanguinarine Cl | 10 ± 1 | NC |
| calmidazolium Cl | 10 ± 1 | Inactive |
| (-)-ephedrine hemisulfate | Inactive | Inactive |
Legend: We subjected Sfp and human PPTase to inhibitors hits from previous assay formats. The two PPTases both demonstrate inhibition with product inhibition analog 2’-deoxy-phosphoadenosinephosphate (2’-deoxy-PAP), product inhibitor PAP and the competitive inhibitor coenzyme A. The compounds with previously identified Sfp inhibitory activity did not demonstrate any significant inhibition of human PPTase. However, some compounds slightly depressed human PPTase labeling, albeit not enough to calculate IC50 values. Compounds appearing to increase PPTase labeling are labeled as activators and were studied in further detail by gel analysis (Figure S22). Compounds displaying a reproducible but very small percent inhibition are not calculated “NC”.