| Name | PFI-1 |
| Description | PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay. |
| Cell Research | To determine dose response, cells are aliquoted into 96-well plate at 5 × 103 cells per well in triplicates. PFI-1 is added by 2- or 4-fold serial dilutions. Cell number is measured 5 days after plating using the CellTiter-Glo Kit and normalized to corresponding vehicle-treated groups. IC50 values are calculated by the GraphPad Prism 5 software using the 4-parameter logistic nonlinear regression model. To calculate the relative growth of cells, averaged cell titers of each group on day 1 are assigned a value of 1. All subsequent cell titer values are normalized accordingly. (Only for Reference) |
| In vitro | In rats, PFI-1, administered intravenously at a dose of 1 mg/kg, exhibits a distribution volume of 1 L/kg and a plasma clearance rate of 18 mL/kg per minute, with a half-life of 1 hour. Orally administered PFI-1 at a dose of 2 mg/kg demonstrates a low efficacy of 32%. When PFI-1 is administered subcutaneously to mice at a 2 mg/kg dose, the peak concentration (Cmax) reaches 58 ng/mL, the time to peak concentration (Tmax) is 1 hour, and the half-life is approximately 2 hours. |
| In vivo | In human monocytes stimulated by lipopolysaccharides, PFI-1 (EC50=1.89 μM) suppresses the production of IL-6. It also inhibits cell proliferation in three NET cell lines (pancreatic NET-derived Bon-1 and lung NET-derived H727 and H720). In T4302 CD133+ cells, PFI-1 induces a dose-dependent decrease in cell viability. PFI-1 (KD=49 μM) binds to the cAMP response element-binding protein. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 40 mg/mL (115.14 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.76 mM), Sonication is recommended.
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| Keywords | PFI-1 | PF6405761 | PF 6405761 | Inhibitor | inhibit | EpigeneticReaderDomain | Epigenetic Reader Domain | BRD4 | BRD2 | Autophagy | Apoptosis |
| Inhibitors Related | Stavudine | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Tributyrin | Paeonol | Naringin | L-Ascorbic acid sodium salt | Alginic acid | Gefitinib | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Reprogramming Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | PPI Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
