1. Metabolic Enzyme/Protease
    Autophagy
  2. Phospholipase
    Autophagy
  3. FIPI

FIPI (Synonyms: 5-Fluoro-2-indolyl deschlorohalopemide)

Cat. No.: HY-12807 Purity: 99.49%
Handling Instructions

FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.

For research use only. We do not sell to patients.

FIPI Chemical Structure

FIPI Chemical Structure

CAS No. : 939055-18-2

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10 mM * 1 mL in DMSO USD 92 In-stock
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10 mg USD 132 In-stock
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50 mg USD 480 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    FIPI purchased from MCE. Usage Cited in: J Cell Sci. 2018 Mar 16;131(6). pii: jcs207217.

    ER:Ras IMR90 cells are treated with solvent or FIPI (250 nM, 2h).Western blotting are performed.

    FIPI purchased from MCE. Usage Cited in: Anal Chem. 2018 Jun 5;90(11):6742-6748.

    Typical CSLM images of MDA-MB-231 cells incubated with 50 μg/mL RhB-PL-Ti3C2 for 4 h at 37°C in the absence (I) and presence of 1.0 mg/mL FIPI (II), and CSLM images of MCF-7 cells (III) incubated with 50 μg/mL RhB-PL-Ti3C2 for 4 h at 37°C.

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    Description

    FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.

    IC50 & Target

    IC50: 25 nM (PLD1), 20 nM (PLD2)

    In Vitro

    Despite the high clearance of greater than 2 L/h/kg, FIPI shows a half-life of greater than 5 h, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%[1]. FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM. FIPI is not an irreversible suicide inhibitor but neither is it rapidly and completely reverses upon removal of the drug. IPI does not alter PLD subcellular localization, access to PIP2, actin stress fibers, or upstream signaling events. FIPI rescues PLD2-suppressed membrane ruffling and cell spreading[2]. FIPI attenuats the thimerosal-induced PLD activation, and the Hg-induced PLD activation in MAECs in a dose-dependent manner, and the agonist- and oxidant-induced PLD activation in a dose-dependent manner in MAECs[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    421.47

    Formula

    C₂₃H₂₄FN₅O₂

    CAS No.

    939055-18-2

    SMILES

    O=C(C(N1)=CC2=C1C=CC(F)=C2)NCCN3CCC(N4C5=CC=CC=C5NC4=O)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 14.67 mg/mL (34.81 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3726 mL 11.8632 mL 23.7265 mL
    5 mM 0.4745 mL 2.3726 mL 4.7453 mL
    10 mM 0.2373 mL 1.1863 mL 2.3726 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [3]

    Phospholipase D activity is quantified using our established method of measuring the formation of [32P]-radiolabeled PBt. Cellular lipids are extracted and PBt is isolated using our published methods of lipid extraction and thin layer chromatographic separation, respectively. Radioactivity is measured using liquid scintillation counting and quantified as DPM normalized to 106 counts in the total cellular lipid extract or as percentage of control (vehicle-treated cells).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Cytotoxicity in MAECs is determined by assaying the extent of reduction in MTT in intact cells using the commercial MTT reduction assay kit. At the end of the experimental treatments, MTT solution (10% vol/vol in MEM) is added and the cells are incubated for 3 hours, following which MTT solvent is added in an amount equal to the original culture volume. Absorbance of the reduced MTT is determined spectrophotometrically, according to the manufacturer's recommendations.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    FIPI5-Fluoro-2-indolyl deschlorohalopemidePhospholipaseAutophagyInhibitorinhibitorinhibit

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