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

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

Cat. No.: HY-15484 Purity: 98.58%
COA
SDS
Handling Instructions Technical Support

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 63208-82-2

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
500 mg 해외재고보유
1 g 해외재고보유
5 g   견적 받기  
10 g   견적 받기  

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고객리뷰

Based on 97 publication(s) in Google Scholar

Other Forms of Pifithrin-α hydrobromide:

Pifithrin-α hydrobromide Related Antibodies

Top Publications Citing Use of Products

97 Publications Citing Use of MCE Pifithrin-α hydrobromide

WB
IF

    Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2023 Mar 13:800:137125.  [Abstract]

    Pifithrin-α hydrobromide (PFT-α; 0.5 μM; 0, 24, 48 h) reverses the inhibition of NSC cell proliferation (SV2A knockdown promotes NSCs apoptosis) (fig C) and reduces cleaved caspase 3 (CC3) expression (fig D) induced by SV2A knockdown.

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

    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 MedChemExpress. Usage Cited in: Am J Cancer Res. 2018 Sep 1;8(9):1697-1711.  [Abstract]

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

    Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Front Genet. 2018 Aug 31:9:320.  [Abstract]

    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.

    • Biological Activity

    • Protocol

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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].

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

    Pifithrin-α hydrobromide Related Antibodies
    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].

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

    367.30

    화학식

    C16H19BrN2OS
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    보관

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    용액&용해도
    In Vitro: 

    DMSO : ≥ 50 mg/mL (136.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7225 mL 13.6127 mL 27.2254 mL
    5 mM 0.5445 mL 2.7225 mL 5.4451 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 몰농도 계산기

    • 농도 희석 계산기

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (27.23 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (27.23 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서

    Purity: 98.58%

    SDS (393 KB)

    COA (255 KB) HNMR (263 KB) RP-HPLC (249 KB) MS (71 KB)

    Handling Instructions (2659 KB)
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7225 mL 13.6127 mL 27.2254 mL 68.0635 mL
    5 mM 0.5445 mL 2.7225 mL 5.4451 mL 13.6127 mL
    10 mM 0.2723 mL 1.3613 mL 2.7225 mL 6.8064 mL
    15 mM 0.1815 mL 0.9075 mL 1.8150 mL 4.5376 mL
    20 mM 0.1361 mL 0.6806 mL 1.3613 mL 3.4032 mL
    25 mM 0.1089 mL 0.5445 mL 1.0890 mL 2.7225 mL
    30 mM 0.0908 mL 0.4538 mL 0.9075 mL 2.2688 mL
    40 mM 0.0681 mL 0.3403 mL 0.6806 mL 1.7016 mL
    50 mM 0.0545 mL 0.2723 mL 0.5445 mL 1.3613 mL
    60 mM 0.0454 mL 0.2269 mL 0.4538 mL 1.1344 mL
    80 mM 0.0340 mL 0.1702 mL 0.3403 mL 0.8508 mL
    100 mM 0.0272 mL 0.1361 mL 0.2723 mL 0.6806 mL
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    Pifithrin-α hydrobromide Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Pifithrin-α63208-82-2PifithrinPFTαMDM-2/p53Aryl Hydrocarbon ReceptorFerroptosisApoptosisAhRInhibitorinhibitorinhibit

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    상품명:
    Pifithrin-α hydrobromide
    Cat. No.:
    HY-15484
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