Phorbol 12-myristate 13-acetate

CAS号

16561-29-8

分子式

C36H56O8

主要靶点

S1P Receptor|NF-κB|PKC

仅限科研使用

Cat No : CM00437

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Synonyms

Sphingosine kinase|SphK|S1PReceptor|S1P Receptor|TPA|佛波醇12-十四酸酯13-乙酸酯|Inhibitor|PKC|PMA|Phorbol myristate|Phorbol 12 myristate 13 acetate|Phorbol 12-myristate|Phorbol 12myristate 13acetate|Phorbol 12-myristate 13-acetate|Protein kinase C|Nuclear factor-κB|Nuclear factor-kappaB|NFκB|NF-κB|NF-kB|NFkB|inhibit



产品信息

CAS号 16561-29-8
分子式 C36H56O8
主要靶点 S1P Receptor|NF-κB|PKC
主要通路 细胞骨架|表观遗传|G 蛋白偶联受体|NF-κB 信号通路
分子量 616.83
纯度 100%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 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 | Shipping with blue ice.
别名 Sphingosine kinase|SphK|S1PReceptor|S1P Receptor|TPA|佛波醇12-十四酸酯13-乙酸酯|Inhibitor|PKC|PMA|Phorbol myristate|Phorbol 12 myristate 13 acetate|Phorbol 12-myristate|Phorbol 12myristate 13acetate|Phorbol 12-myristate 13-acetate|Protein kinase C|Nuclear factor-κB|Nuclear factor-kappaB|NFκB|NF-κB|NF-kB|NFkB|inhibit

靶点活性

PKC:11.7 nM (EC50)

体内活性

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]

体外活性

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]

溶解度

10% DMSO+40% PEG300+5% Tween 80+45% Saline:6 mg/mL (9.73 mM);DMSO:60 mg/mL (97.27 mM);H2O:Insoluble

细胞实验

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].

动物实验

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].

参考文献

1.J?rgensen 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.

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