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Phorbol 12-myristate 13-acetate
Catalog No. TQ0198 CAS 16561-29-8
Synonyms: PMA
Phorbol 12-myristate 13-acetate (PMA) belongs to the phorbol ester group of natural products and is an activator of PKC, SphK, and NF-κB. Phorbol 12-myristate 13-acetate induces THP1 cell differentiation.
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Phorbol 12-myristate 13-acetate, CAS 16561-29-8
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1 mg
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50 mg
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1 mL * 10 mM (in DMSO)
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Purity: 100%
Purity: 99.87%
Purity: 99.5%
Purity: 99.07%
Purity: 98.55%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description
Phorbol 12-myristate 13-acetate (PMA) belongs to the phorbol ester group of natural products and is an activator of PKC, SphK, and NF-κB. Phorbol 12-myristate 13-acetate induces THP1 cell differentiation.
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]
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].
Source
Natural Products > Euphorbiaceae > Euphorbia
Synonyms
PMA
Molecular Weight
616.83
Formula
C36H56O8
CAS No.
16561-29-8
Storage
store at low temperature,keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 60 mg/mL (97.27 mM)
H2O: Insoluble
References and Literature
1. Jørgensen K, et al. Phorbol ester phorbol-12-myristate-13-acetate promotes anchorage-independent growth and survival of melanomas through MEK-independent activation of ERK1/2. Biochem Biophys Res Commun. 2005 Apr 1;329(1):266-74. 2. Starr T, et al. The phorbol 12-myristate-13-acetate differentiation protocol is critical to the interaction of THP-1 macrophages with Salmonella Typhimurium. PLoS One. 2018 Mar 14;13(3):e0193601. 3. Wen HC, et al. PMA inhibits endothelial cell migration through activating the PKC-δ/Syk/NF-κB-mediated up-regulation of Thy-1. Sci Rep. 2018 Nov 2;8(1):16247. 4. Dzietko M, et al. Effects of PMA (PHORBOL-12-MYRISTATE-13-ACETATE) on the Developing Rodent Brain. Biomed Res Int. 2015;2015:318306. 5. Wu BC, et al. In vivo Anti-inflammatory Activity of Lipidated Peptidomimetics Pam-(Lys-βNspe)6-NH2 and Lau-(Lys-βNspe)6-NH2 Against PMA-Induced Acute Inflammation. Front Immunol. 2020 Aug 28;11:2102.
Citations
1. Chen H, Duan X, Deng X, et al.EBV-upregulated B7-H3 inhibits NK cell–mediated antitumor function and contributes to nasopharyngeal carcinoma progression.Cancer Immunology Research.2023: CIR-22-0374. 2. Hu R, Molibeli K M, Zhu L, et al.Long non-coding RNA-XLOC_002383 enhances the inhibitory effects of THP-1 macrophages on M. avium and functions as a competing endogenous RNA by sponging miR-146a-5p to target TRAF6.Microbes and Infection.2023: 105175. 3. Hu H, Jiang H, Zhang K, et al. Memantine nitrate MN-08 suppresses NLRP3 inflammasome activation to protect against sepsis-induced acute lung injury in mice. Biomedicine & Pharmacotherapy. 2022, 156: 113804 4. Li Y, Wu Y, Li S, et al. Identification of phytochemicals in Qingfei Paidu decoction for the treatment of coronavirus disease 2019 by targeting the virus-host interactome. Biomedicine & Pharmacotherapy. 2022: 113946. 5. Yasin Z N M, Idrus F N M, Yvonne-Tee G B.Comparison of THP-1 Macrophages Viability in Different Types of Culture Vessel.Journal of Tropical Life Science.2023, 13(2): 359-368. 6. Wu M, Shi Y, Liu Y, et al.Exosome‐transmitted podoplanin promotes tumor‐associated macrophage‐mediated immune tolerance in glioblastoma.CNS Neuroscience & Therapeutics.2024, 30(3): e14643. 7. Zhang Y, Shi Q, Wang P, et al.iPSC‐derived NK cells with site‐specific integration of CAR19 and IL24 at the multi‐copy rDNA locus enhanced antitumor activity and proliferation.MedComm.2024, 5(5): e553.
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL),
Method for preparing in vivo formulation:Take μL DMSO master liquid, next add μL PEG300, mix and clarify, next add μL Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL DMSO master liquid, next add μL Corn oil,mix and clarify.
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