PFI-1

SKU: orb1300965

Description

PFI-1 (PF-6405761) is a potent and selective BET bromodomain inhibitor, exhibiting an IC50 of 0.22 µM against BRD4 in biochemical assays. This cell-permeable compound is a valuable chemical probe for investigating BET protein function in cancer, inflammation, and transcriptional regulation in both cellular and animal models.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1403764-72-6
• MW: 347.39
• Purity: 99.19%
• Formula: C₁₆H₁₇N₃O₄S
• SMILES: COc1ccccc1S(=O)(=O)Nc1ccc2NC(=O)N(C)Cc2c1
• Target: Autophagy,Apoptosis,Epigenetic Reader Domain
• Solubility: DMSO:40 mg/mL (115.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.76 mM)

Bioactivity

• Target IC50:
  BRD4:0.22 μM
• 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.
• 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.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, Autophagy, BRD2, BRD4, Epigenetic Reader Domain, EpigeneticReaderDomain, Inhibitor, inhibit, PF6405761, PF-6405761, PFI1, PFI-1, PFI 1, PF 6405761

Compound Identifiers

PubChem CID

71271629