PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM.
 |
Source | Viruses (2017). Figure 1. PR-619 |
| Method | western blotting | |
| Cell Lines | HeLa cells | |
| Concentrations | 20 μM | |
| Incubation Time | 24 h | |
| Results | Densitometric analyses of the western blot data illustrate that the efficacy of Gag processing was reduced by about 2-fold in cells treated with P22077 or PR-619, whereas cells treated with the DI P5091 had wt level, indicating that certain DUB activities regulate late steps of HIV replication. |
| Molecular Weight | 223.28 |
| Formula | C7H5N5S2 |
| CAS Number | 2645-32-1 |
| Solubility (25°C) | DMSO 21 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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