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  4. Phorbol 12-myristate 13-acetate

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

Cat. No.: HY-18739 Purity: 99.80%
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Phorbol 12-myristate 13-acétate (PMA), un ester de phorbol, est un activateur double SphK et protéine kinase C (PKC).

Phorbol 12-Myristat 13-Acetat (PMA), ein Phorbolester, ist ein doppelter SphK- und Proteinkinase C (PKC) -Aktivator.

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.

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

CAS No. : 16561-29-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 392 publication(s) in Google Scholar

Top Publications Citing Use of Products

MedChemExpress Activity Verification

Above results were obtained through MCE biological verification.

389 Publications Citing Use of MCE Phorbol 12-myristate 13-acetate

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).

    MCE Biological Validation

    WB
    Cell Culture
      THP-1 cells were seeded at 2 × 105 cells/well in a 24 well plate and treated with 100 and 200 ng/mL Phorbol 12-myristate 13-acetate (PMA) (HY-18739) for 24 h. Cells were lysed and the expression of CD11b was measured. The results indicated that PMA increases expression of CD11b.
      THP-1 cells were seeded at 2 × 105 cells/well in a 24 well plate and treated with 100 and 200 ng/mL Phorbol 12-myristate 13-acetate (PMA) (HY-18739) for 24 or 48 h. The results indicated that PMA induces THP-1 cell differentiation.

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      • Biological Activity

      • Protocol

      • Purity & Documentation

      • References

      • Customer Review

      Description

      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

       

      Cellular Effect
      Cell Line Type Value Description References
      MT4 EC50
      0.7 nM
      Compound: 13
      Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
      Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
      [PMID: 25970561]
      MT4 EC50
      0.9 nM
      Compound: 13
      Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
      Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
      [PMID: 25970561]
      SNU-387 IC50
      > 10 μM
      Compound: 10
      Cytotoxicity against human SNU387 cells after 48 hrs by MTT assay
      Cytotoxicity against human SNU387 cells after 48 hrs by MTT assay
      [PMID: 23701597]
      U-937 EC50
      0.45 nM
      Compound: PMA
      Induction of attachment of U937 cells after 48 hrs
      Induction of attachment of U937 cells after 48 hrs
      [PMID: 17284021]
      Vero EC50
      > 162 μM
      Compound: 4, TPA
      Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      [PMID: 23215460]
      Vero EC50
      0.0029 μM
      Compound: 4, TPA
      Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      [PMID: 23215460]
      Vero EC50
      2.2 μM
      Compound: 4, TPA
      Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
      [PMID: 23215460]
      Vero EC50
      2.9 nM
      Compound: 13
      Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
      Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
      [PMID: 25970561]
      Vero CC50
      5.7 μM
      Compound: 4, TPA
      Cytotoxicity against african green monkey Vero cells by MTS assay
      Cytotoxicity against african green monkey Vero cells by MTS assay
      [PMID: 23215460]
      Vero CC50
      5.7 μM
      Compound: TPA
      Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method
      Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method
      [PMID: 28925702]
      In Vitro

      PMA (100, 200 ng/mL; 1-5 days) induce THP-1 cells to differentiate into macrophage-like cells (THP-1 macrophages), characterized by changes in morphology (adherent macrophage-like phenotype), and increases cell surface expression of CD11b[3][5].
      PMA (20 ng/mL, 36 h) inhibits endothelial cell migration through activating the PKC-δ/Syk/NF-κB-mediated up-regulation of Thy-1[8].

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

      In Vivo

      Phorbol 12-myristate 13-acetate (PMA) can be used to create models of ear edema and paw edema[8][9].

      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
      Note
      Modeling Indicators
      Appearance monitoring: The thickness difference between the left and right ears increases significantly.
      Indicator changes: Increased vascular permeability.
      Correlated Product(s): /
      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
      Rat: 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.
      Opposite Product(s): /

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

      Molecular Weight

      616.83

      Formula

      C36H56O8

      CAS No.
      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
      Shipping

      Room temperature in continental US; may vary elsewhere.

      Storage

      -20°C, protect from light

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

      Solvent & Solubility
      In Vitro: 

      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
      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.

      • Molarity Calculator

      • Dilution Calculator

      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)

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      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 (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:

      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 (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.
      Purity & Documentation

      Purity: 99.80%

      References
      Cell Assay
      [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].

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

      Animal Administration
      [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.

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

      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 (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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      Product Name:
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