1. Apoptosis
    Immunology/Inflammation
  2. MDM-2/p53
    Aryl Hydrocarbon Receptor
  3. Pifithrin-α hydrobromide

Pifithrin-α hydrobromide (Synonyms: Pifithrin hydrobromide; PFTα hydrobromide)

Cat. No.: HY-15484 Purity: 98.28%
Handling Instructions

Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.

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

Pifithrin-α hydrobromide Chemical Structure

Pifithrin-α hydrobromide Chemical Structure

CAS No. : 63208-82-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
25 mg USD 204 In-stock
Estimated Time of Arrival: December 31
50 mg USD 324 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Top Publications Citing Use of Products

    Pifithrin-α hydrobromide purchased from MCE. Usage Cited in: Mol Nutr Food Res. 2018 Aug;62(16):e1800164.

    PFT-α, a pharmacological p53 inhibitor, inhibits the expression of frataxin in HepG2 cells. Under the treatment of free fatty acids (FFAs), the frataxin are further decreased by PFT-α.

    Pifithrin-α hydrobromide purchased from MCE. Usage Cited in: Front Genet. 2018 Aug 31;9:320.

    Western blot analysis of the expression of p53 and caspase-3 after intrathecal administration of Pifithrin-α on day 7 after chronic constriction injury (CCI). The fold change of p53 and caspase-3 levels is normalized to the glyceraldehyde 3-phosphate dehydrogenase (GAPDH) level.

    Pifithrin-α hydrobromide purchased from MCE. Usage Cited in: Am J Cancer Res. 2018 Sep 1;8(9):1697-1711.

    Pifithrin-α hydrobromide (PFT) treatment inhibits Atovaquone (ATO)-induced upregulation of p53, p21, and cleavage of PARP, as well as downregulation of CDK2.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.

    IC50 & Target

    p53[1]
    AhR[2]

    In Vitro

    Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect. Notably, Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates[1]. Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and. Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex, activate reporter activity, and up-regulate the classic AhR target gene CYP1A1[2].

    In Vivo

    When the experiment is performed with Pifthirin-α (PFT-α) hydrobromide, a pharmacological p53 inhibitor, the percentage of annexin V-positive Foxe3-/- SMCs decreases to WT levels. Pifithrin-α (2.2 mg/kg, i.p.) significantly reduces the incidence of aortic rupture and intramural hematomas in Foxe3-/- mice that underwent transverse aortic constriction (TAC) (50% to 17%, P<0.05). After Pifthirin-α treatment, the mean diameter of the ascending aorta and the percentage of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals (P<0.05)[3].

    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 : ≥ 50 mg/mL (136.13 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7226 mL 13.6129 mL 27.2257 mL
    5 mM 0.5445 mL 2.7226 mL 5.4451 mL
    10 mM 0.2723 mL 1.3613 mL 2.7226 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice, resuspended in 0.2 mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone[2].

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

    Cell Assay
    [1]

    The human hepatoma cell lines HepG2 (p53++) are cultured in RMPI 1640 medium with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37°C in an atmosphere containing 5% CO2. Cells are exposed to GOX (0-5 0U) for 0-8 hours with or without Pifithrin-α (20 μM/L), Pifithrin-μ (5 μM/L), CsA (10 μM/L), Sanglifehrin A (20 μM/L) and NAC (5 mM/L) for 1 hour, respectively. After treatment, cells are collected and processed for further experiments[1].

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

    Animal Administration
    [3]

    Mice[3]
    The Foxe3-null (Foxe3-/-) mice are used. To investigate the role of p53 in Foxe3-related apoptosis, Pifithrin-α is administered by i.p. injection at a dosage of 2.2 mg/kg, then dissolved in PBS 1 hour before TAC and then every 48 hours. Animals are euthanized 2 weeks after the surgery, and the ascending aortic tissues are harvested for either RNA, total protein, histomorphometric analysis, or TUNEL assay.

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

    References
    Molecular Weight

    367.30

    Formula

    C₁₆H₁₉BrN₂OS

    CAS No.

    63208-82-2

    SMILES

    N=C1SC2=C(CCCC2)N1CC(C3=CC=C(C)C=C3)=O.[H]Br

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Pifithrin-α hydrobromide
    Cat. No.:
    HY-15484
    Quantity:

    Pifithrin-α hydrobromide

    Cat. No.: HY-15484