Phorbol 12-myristate 13-acetate

SKU: orb1296136

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.

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 16561-29-8
• MW: 616.83
• Purity: 99.58%
• Formula: C₃₆H₅₆O₈
• SMILES: [H][C@]12[C@]3([H])C=C(CO)C[C@]4(O)C(=O)C(C)=C[C@@]4([H])[C@@]3(O)[C@H](C)[C@@H](OC(=O)CCCCCCCCCCCCC)[C@@]1(OC(C)=O)C2(C)C
• Target: PKC,NF-κB,S1P Receptor
• Solubility: DMSO: 60 mg/mL (97.27 mM), Sonication is recommended. H2O: Insoluble

Bioactivity

• Target IC50:
  PKC:11.7 nM (EC50)
• In Vivo:
  METHODS: To investigat 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, an 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. 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.
• 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 usin the MTS. Results: Phorbol 12-myristate 13-acetate promote the proliferation of melanoma cells, an the cell number of WM35 cells increased to 265%. 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 surfacee expression of CD11 and CD14 was increased. 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 usin the Wound healing migration assay. Results: Short-term treatment with Phorbol 12-myristate 13-acetate enhanced endothelial cell migration.
• Cell Research:
  αT3-1 and LβT-2 cells are grown in monolayer cultured in DMEM in humidified incubator 5% CO2 at 37℃. Serum starvation is with 0.1% FCS in the same medium for 16 h. GnRH and PMA are then added fo 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 o 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 o 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 wit the lysis buffer, followed by one freeze-thaw cycle. Cells are Harvested; following centrifugation (15,00 × , 15 min, 4°C) supernatants are taken for immunoprecipitation experiments.
• Animal Research:
  All experiments are performed with Male Wistar rats (weighing 250-280 g). One hundred and thirty-five Wistar rats are andomly divided into seven groups. (1) Rats in the sham group ( = 1) are given a lateral cerebral ventricle injection of 0.9% normal saline; (2) Rats in the IR group ( = 1) 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 ( = 1) are given a lateral cerebral ventricle injection of CBX (5 μg/m × 0 μL) 30 min before MCAO; (4) Rats in the Sch-6783 group ( = 1) 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 ( = 1) are given a lateral cerebral ventricle injection of 5 hD (100 m × 0 μL), and after 10 min, DZX is injected 15 min prior to MCAO; (6 the rats in the DZX + Ro group ( = 5) 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 ( = 5) are given an intraperitoneal injection of PMA (200 μg/kg) afte the injection of 5 hD and DZX.

Storage & Handling

• 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.
• Disclaimer: For research use only

Alternative Names

Protein kinase C, S1PReceptor, S1P Receptor, TPA, SphK, Sphingosine kinase, PKC, Phorbol 12 myristate 13 acetate, Phorbol 12-myristate, Phorbol 12myristate 13acetate, Phorbol 12-myristate 13-acetate, Phorbol myristate, Nuclear factor-kappaB, Nuclear factor-κB, PMA, NFκB, NF-κB, NFkB, NF-kB, Inhibitor, inhibit

Compound Identifiers

PubChem CID

27924