PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM.
 |
Source | Sci Rep (2017). Figure 1. PFI-1 |
| Method | flow cytometry | |
| Cell Lines | C11 cells or A10.6 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24 to 72 h | |
| Results | To determine the effect of RVX-208 and PFI-1 on latent HIV-1 reactivation, we used J-Lat C11 cell line in which transcriptional activation of the latent provirus can be detected in individual cells by flow cytometry, since these cells harbor full-length latent HIV-1 provirus containing GFP gene in place of nef |
| Molecular Weight | 347.39 |
| Formula | C16H17N3O4S |
| CAS Number | 1403764-72-6 |
| Solubility (25°C) | DMSO 18 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.
[4] Panpan Lu, et al. BET inhibitors RVX-208 and PFI-1 reactivate HIV-1 from latency
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