Phorbol 12-myristate 13-acetate Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

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.
In vitro	方法：球体培养的人类黑色素瘤细胞 WM 系列用 Phorbol 12-myristate 13-acetate (50 ng/mL) 处理 3 天，使用 MTS 方法检测细胞生长情况。结果：Phorbol 12-myristate 13-acetate 促进黑色素瘤细胞增殖，WM35 细胞的细胞数提高到 265%。[1]方法：人单核白血球细胞 THP-1 用 Phorbol 12-myristate 13-acetate (200 ng/mL) 处理 1-5 天，使用光学显微镜评估形态，使用 Flow Cytometry 方法检测靶点表达。结果：Phorbol 12-myristate 13-acetate 诱导 THP-1 细胞分化为巨噬细胞样细胞 (THP-1 巨噬细胞)，CD11 和 CD14 的细胞表面表达增加。[2]方法：人静脉内皮细胞 HUVECs 用 Phorbol 12-myristate 13-acetate (10-40 ng/mL) 处理 8 h，使用 Wound healing migration assay 检测细胞迁移情况。结果：短期 Phorbol 12-myristate 13-acetate 处理可增强内皮细胞迁移。[3]
In vivo	方法：为研究佛波酯对啮齿类动物大脑发育的影响，将 Phorbol 12-myristate 13-acetate (100-500 μg/kg) 单次腹腔注射给药给缺乏 IL-18 或 IRAK-4 的新生大鼠和小鼠，24 h、7 天或14 天后处死动物。结果：Phorbol 12-myristate 13-acetate 在大脑中诱导炎症反应并引起广泛的神经退行性变。缺乏 IL-18 或 IRAK-4 对 Phorbol 12-myristate 13-acetate 诱导的脑损伤有保护作用。[4]方法：为构建急性小鼠耳炎症模型，将 Phorbol 12-myristate 13-acetate (20 μL 125 μg/mL PMA 丙酮溶液) 局部处理 CD-1 小鼠双耳，风干并完全吸收。结果：用 Phorbol 12-myristate 13-acetate 攻击的耳组织在施用约 2 小时开始出现炎症迹象，包括肿胀和发红。[5]
Cell experiments	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 experiments	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].
Target activity	PKC:11.7 nM (EC50)
Synonyms	佛波醇12-十四酸酯13-乙酸酯, PMA
molecular weight	616.83
Molecular formula	C36H56O8
CAS	16561-29-8
Storage	keep away from direct sunlight,store under nitrogen,store at low temperature　\|　Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	DMSO: 60 mg/mL (97.27 mM) H2O: Insoluble
References	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. 8. Jiang J, Shen W, He Y, et al.Overexpression of NLRP12 enhances antiviral immunity and alleviates herpes simplex keratitis via pyroptosis/IL-18/IFN-γ signaling.International Immunopharmacology.2024, 137: 112428. 9. Yin L, Zhang E, Mao T, et al.Macrophage P2Y6R activation aggravates psoriatic inflammation through IL-27-mediated Th1 responses.Acta Pharmaceutica Sinica B.2024

PeptideDB

Phorbol 12-myristate 13-acetate

CAS No.: 16561-29-8