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  5. Phorbol 12-myristate 13-acetate

Phorbol 12-myristate 13-acetate  (Synonyms: PMA; TPA; Phorbol myristate acetate)

製品番号: HY-18739 純度: 99.07%
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Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells.

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Phorbol 12-myristate 13-acetate 構造式

Phorbol 12-myristate 13-acetate 構造式

CAS 番号 : 16561-29-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 147 在庫あり
Solid
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5 mg USD 108 在庫あり
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Based on 246 publication(s) in Google Scholar

Phorbol 12-myristate 13-acetate 関連抗体

Top Publications Citing Use of Products

顧客検証

WB

    Phorbol 12-myristate 13-acetate purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2019 Apr;142:1-13.  [Abstract]

    Total lysates from cells are analyzed for the expression of MMP-2 and MMP-9 by Western blot analysis in the treatment of different concentrations of PMA and PDD.

    Phorbol 12-myristate 13-acetate purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2019 Apr;142:1-13.  [Abstract]

    MDA-MB-231 cells are pretreated with PPD for 24 h followed by exposure to 50 ng/mL of PMA for 30 min. The whole cell lysates are analyzed by Western blot for the activation of MAPK.

    Phorbol 12-myristate 13-acetate purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2017 Aug 7;10:247.  [Abstract]

    Bar graphs show levels of GABAAR-α2 mRNA and GABAAR-α2 protein in BLA of control mice treated with BLA-injection of H89 or GF109203X (GFX); in MPTP-mice treated with BLA-injection of PMA, or the co-administration of quinpirole and H89 (quin/+H89) or GF109203X (quin/+GFX).

    PKC アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

    NF-κB アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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    製品説明

    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator[1][2]. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells[3][7].

    IC50 & Target[1][7]

    PKC

    11.7 nM (EC50)

    NF-κB

     

    体外実験

    In order to examine the role of PKC in p38MAPK phosphorylation, the cells are stimulated with the PKC activator, Phorbol 12-myristate 13-acetate (PMA) (100 nM), which mimics the binding of DAG, the natural activator of PKC, to the C1 region of the PKCs. p38MAPK phosphorylation by PMA is observed in the two cell types similar to that observed by GnRH in αT3-1 cells, that is, a slow sustained activation (3.2-fold and 3.6-fold, respectively at 30 min). The paradoxical findings that PKCs activated by GnRH and PMA play a differential role in p38MAPK phosphorylation may be explained by differential localization of the PKCs. Basal, GnRH- and PMA- stimulation of p38MAPK phosphorylation in αT3-1 cells is mediated by Ca2+ influx via voltage-gated Ca2+ channels and Ca2+ mobilization, while in the differentiated LβT2 gonadotrope cells it is mediated only by Ca2+ mobilization[2].
    THP-1 cells are differentiated into macrophage-like cells (THP-1 macrophages) by incubation in the presence of PMA (200 ng/mL; 1-5 days), which leads to a macrophage-like phenotype characterized by changes in morphology and increased cell surface expression of CD11 and CD14[3].
    In the monocytic cell line THP-1, PMA results in a more differentiated phenotype than VD3, according to adherence, loss of proliferation, phagocytosis of latex beads, and expression of CD11b and CD14[5].

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

    Phorbol 12-myristate 13-acetate 関連抗体
    体内実験

    Phorbol 12-myristate 13-acetate can be used in animal modeling to construct eczema-like models. Phorbol 12-myristate 13-acetate (PMA) is a PKC agonist, which reverses the damage induced by 5-hydroxydecanoic acid (5-HD). Thus, activation of the mitoKATP protected mitochondrial function in SOD and MDA via the PKC pathway[4].
    1. Induction of oedema at ear[8]
    Background
    PMA induces a pronounced inflammatory response mediated by protein kinase C (PKC), specifically activating PLA2 to trigger inflammation.
    Specific Mmodeling Methods
    Mice: Swiss mouse • Female • 25-30 g
    Administration: Topically applied in one ear • 100 μg/mL in 20 μL (2 μg/ear) vehicle • single dose


    Modeling Indicators
    Appearance monitoring: The thickness difference between the left and right ears increases significantly.
    Indicator changes: Increased vascular permeability.
    Opposite Product(s): Hydroxyachillin; Indomethacin (HY-14397)
    2. Induction of oedema at feet[9]
    Background
    PMA induces a pronounced inflammatory response mediated by protein kinase C (PKC), specifically activating PLA2 to trigger inflammation.
    Specific Mmodeling Methods
    Rats: Wistar • male • adult with weight of 200-220 g
    Mice: Swiss albino • male • 25-30 g
    Administration: Topically applied in one ear • 2.5 μg in 20 μL vehicle • single dose
    Note
    Administration should be conducted 4 h before mouse were killed.


    Modeling Indicators
    Appearance monitoring: The quality difference between the left and right ears increases significantly.
    Indicator changes: Stimulate macrophages to produce superoxide anions.
    Correlated Product(s): Carrageenan (HY-125474); Histamine (HY-B1204); Serotonin (HY-B1473A); Prostaglandin E2 (PGE2) (HY-101952)
    Opposite Product(s):

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

    616.83

    分子式

    C36H56O8
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCCCCCCCCCCCC(O[C@H]([C@H]1C)[C@]2(OC(C)=O)[C@@]([C@@](C=C(CO)C[C@]34O)([H])[C@@]1(O)[C@]4([H])C=C(C)C3=O)([H])C2(C)C)=O
    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (162.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 100 mg/mL (162.12 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6212 mL 8.1060 mL 16.2119 mL
    5 mM 0.3242 mL 1.6212 mL 3.2424 mL
    10 mM 0.1621 mL 0.8106 mL 1.6212 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    体内:

    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 (4.05 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 (4.05 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

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    Dosing volume
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    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 (protect from light)

    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.
    純度とドキュメンテーション

    純度: 99.66%

    COA (247 KB) HNMR (201 KB) LCMS (122 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [2]

    αT3-1 and LβT-2 cells are grown in monolayer cultured in DMEM in humidified incubator 5% CO2 at 37°C. Serum starvation is with 0.1% FCS in the same medium for 16 h. GnRH and PMA are then added for the length of time as indicated. In general, αT3-1 cells are transiently transfected by ExGen 500 or by jetPRIME, while LβT2 cells only by jetPRIME transfection reagent. For experiments with dominant-negative (DN) PKCs, αT3-1 cells (in 6 cm plates) are transfected with 1.5 μg of p38α-GFP with 3 μg of control vector, pCDNA3, or with 3 μg of the DN-PKCs constructs. For LβT2 cells, transfections are performed (in 10 cm plates) with 4 μg of p38α-GFP along with 9 μg of control vector, pCDNA3, or with 9 μg of the DN-PKCs constructs. Approximately 30 h after transfection, the cells are serum starved (0.1% FCS) for 16 h and later stimulated with GnRH or PMA, washed twice with ice-cold PBS, treated with the lysis buffer, followed by one freeze-thaw cycle. Cells are harvested; following centrifugation (15,000×g, 15 min, 4°C) supernatants are taken for immunoprecipitation experiments[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [3]

    Rats[3]
    All experiments qre performed with male Wistar rats (weighing 250-280 g). One hundred and thirty-five Wistar rats are randomly divided into seven groups. (1) Rats in the sham group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline; (2) Rats in the IR group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline 30 min before middle cerebral artery occlusion (MCAO); (3) Rats in the Carbenoxolone (CBX) group (n=21) are given a lateral cerebral ventricle injection of CBX (5 μg/mL×10 μL) 30 min before MCAO; (4) Rats in the Sch-6783 group (n=21) are given a lateral cerebral ventricle injection of DZX (2 mM×30 μL) 30 min prior to MCAO; (5) Rats in the 5-HD group (n=21) are given a lateral cerebral ventricle injection of 5-HD (100 mM×10 μL), and after 10 min, DZX is injected 15 min prior to MCAO; (6) The rats in the DZX + Ro group (n=15) are given a lateral cerebral ventricle injection of DZX, and after 10 min, Ro-31-8425 (400 μg/kg) is injected 15 min prior to MCAO; (7) The rats in the 5-HD+PMA group (n=15) are given an intraperitoneal injection of PMA (200 μg/kg) after the injection of 5-HD and DZX.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 (protect from light). 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 / Ethanol 1 mM 1.6212 mL 8.1060 mL 16.2119 mL 40.5298 mL
    5 mM 0.3242 mL 1.6212 mL 3.2424 mL 8.1060 mL
    10 mM 0.1621 mL 0.8106 mL 1.6212 mL 4.0530 mL
    15 mM 0.1081 mL 0.5404 mL 1.0808 mL 2.7020 mL
    20 mM 0.0811 mL 0.4053 mL 0.8106 mL 2.0265 mL
    25 mM 0.0648 mL 0.3242 mL 0.6485 mL 1.6212 mL
    30 mM 0.0540 mL 0.2702 mL 0.5404 mL 1.3510 mL
    40 mM 0.0405 mL 0.2026 mL 0.4053 mL 1.0132 mL
    50 mM 0.0324 mL 0.1621 mL 0.3242 mL 0.8106 mL
    60 mM 0.0270 mL 0.1351 mL 0.2702 mL 0.6755 mL
    80 mM 0.0203 mL 0.1013 mL 0.2026 mL 0.5066 mL
    100 mM 0.0162 mL 0.0811 mL 0.1621 mL 0.4053 mL
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    Phorbol 12-myristate 13-acetate Related Classifications

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    Keywords:

    Phorbol 12-myristate 13-acetate16561-29-8PMA TPAPhorbol myristatePKCSphKNF-κBProtein kinase CSphingosine kinaseNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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