Tamanho : 5mg
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Synonyms: PMA
| Description | Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models. |
| Targets & IC50 | PKC:11.7 nM (EC50) |
| In vitro | METHODS: Sphere-cultured human melanoma cells WM series were treated with Phorbol 12-myristate 13-acetate (50 ng/mL) for 3 days, and cell growth was examined using the MTS. RESULTS: Phorbol 12-myristate 13-acetate promoted the proliferation of melanoma cells, and the cell number of WM35 cells increased to 265%. [1] METHODS: Human mononuclear leukocytes THP-1 were treated with Phorbol 12-myristate 13-acetate (200 ng/mL) for 1-5 days, and morphology was assessed using light microscopy and target expression was detected using Flow Cytometry. RESULTS: Phorbol 12-myristate 13-acetate induced THP-1 cells to differentiate into macrophage-like cells (THP-1 macrophages). Cell surface expression of CD11 and CD14 was increased. [2] METHODS: Human venous endothelial cells HUVECs were treated with Phorbol 12-myristate 13-acetate (10-40 ng/mL) for 8 h. Cell migration was detected using the Wound healing migration assay. RESULTS: Short-term treatment with Phorbol 12-myristate 13-acetate enhanced endothelial cell migration. [3] |
| In vivo | METHODS: To investigate the effects of phorbol esters on rodent brain development, Phorbol 12-myristate 13-acetate (100-500 μg/kg) was administered as a single intraperitoneal injection to neonatal rats and mice deficient in IL-18 or IRAK-4, and the animals were necropsied 24 h, 7 days, or 14 days later. RESULTS: Phorbol 12-myristate 13-acetate induced an inflammatory response and extensive neurodegeneration in the brain. Lack of IL-18 or IRAK-4 protected against Phorbol 12-myristate 13-acetate-induced brain damage. [4] METHODS: To construct an acute mouse ear inflammation model, both ears of CD-1 mice were treated topically with Phorbol 12-myristate 13-acetate (20 μL of 125 μg/mL PMA acetone solution), air-dried and completely absorbed. RESULTS: Ear tissues attacked with Phorbol 12-myristate 13-acetate began to show signs of inflammation, including swelling and redness, approximately 2 hours after application. [5] |
| Synonyms | PMA |
| Disease Modeling Protocol | Precancerous Skin Lesions and Tumor Model
*Precautions： All mice had their back hair shaved 3-7 days prior to the experiment to ensure the drug came into contact with the epidermis. *References：Muller-Decker K,et,al. Transgenic cyclooxygenase-2 overexpression sensitizes mouse skin for carcinogenesis. Proc Natl Acad Sci U S A. 2002 Sep 17;99(19):12483-8. |
| Cell Research | 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]. |
| Animal Research | All experiments are 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 [3]. |
| Molecular Weight | 616.83 |
| Formula | C36H56O8 |
| Cas No. | 16561-29-8 |
| Smiles | 20[C@]12[C@]3(20)C=C(CO)C[C@]4(O)C(=O)C(C)=C[C@@]4(20)[C@@]3(O)[C@H](C)[C@@H](OC(=O)CCCCCCCCCCCCC)[C@@]1(OC(C)=O)C2(C)C |
| Relative Density. | 1.17 g/cm3 |
| Storage | Keep away from direct sunlight,Store under nitrogen,Store at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (97.27 mM), Sonication is recommended.  H2O: Insoluble | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (9.73 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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