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12-O-tetradecanoyl phorbol-13-acetate (PMA)

现货
Catalog No.
N2060
ERK/MAPK激活剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,100.00
Ship with 7 days

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Background

12-O-tetradecanoyl phorbol-13-acetate (TPA) is an activator of ERK/MAPK with the concentration of 50μm [1].

ERK is an extracellular signal-regulated kinase and transfers signals from a receptor on the cell surface to DNA cooperated with MAPK. It is reported that ERK deficiency leads to the cell uncontrolled growth and is regarded as a target to cure cancers.

TPA is a potent ERK activator. When tested with A549 cells (human lung cancer cell line), TPA treatment led to an early, strong, and relatively transient ERK phosphorylation [2]. In mouse embryo fibroblasts from DUSP5 (+/+) mice, administration of TPA increased levels of ERK expression [3].

In transgenic (Eisuke) mice expressing a F?rster resonance energy transfer (FRET) biosensor for ERK, ERK activity was gradually stimulated upon topical TPA treatment and reached the peak approximately 6 hr later [1].

It is also reported that TPA treatment increased the accumulation of immature myeloid cells and the formation of papillomas during epidermal carcinogenesis (important in the tumor formation) when tested with S100A9 transgenic mice [4].

References:
[1].  Hiratsuka, T., et al., Intercellular propagation of extracellular signal-regulated kinase activation revealed by in vivo imaging of mouse skin. Elife, 2014. 4.
[2].  Refsnes, M., et al., Differential NF-kappaB and MAPK activation underlies fluoride- and TPA-mediated CXCL8 (IL-8) induction in lung epithelial cells. J Inflamm Res, 2014. 7: p. 169-85.
[3].  Rushworth, L.K., et al., Dual-specificity phosphatase 5 regulates nuclear ERK activity and suppresses skin cancer by inhibiting mutant Harvey-Ras (HRasQ61L)-driven SerpinB2 expression. Proc Natl Acad Sci U S A, 2014. 111(51): p. 18267-72.
[4].  Ortiz, M.L., et al., Immature myeloid cells directly contribute to skin tumor development by recruiting IL-17-producing CD4+ T cells. J Exp Med, 2015.

文献引用

1.Li L, Ge C, et al. "Dehydroepiandrosterone reduces accumulation of lipid droplets in primary chicken hepatocytes by biotransformation mediated via the cAMP/PKA-ERK1/2 signaling pathway." Biochim Biophys Acta. 2018 Mar 20;1863(6):625-638. PMID:29571766

Chemical Properties

StorageStore at -20°C
M.Wt616
Cas No.16561-29-8
FormulaC36H56O8
Solubility≥112.9mg/mL in DMSO
SDFDownload SDF
Canonical SMILESCCCCCCCCCCCCCC(=O)OC1C(C2(C(C=C(CC3(C2C=C(C3=O)C)O)CO)C4C1(C4(C)C)OC(=O)C)O)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

酶学实验 [1]:

激酶检测

通过测量从[γ-32P] ATP将32P掺入H1组蛋白中来测定蛋白激酶C。反应混合物(0.25ml)含有5pmol Tris-HCl,pH7.5,1.25pmol硝酸镁,50μgH1组蛋白,2.5nmol [γ-32P] ATP(5~15x104 cpm/nmol)和0.5pg蛋白激酶C。加入磷脂,二油烯,佛波酯和Ca2+作为指示剂。所有试剂在双蒸馏水中制备,然后通过Chelex 100柱以尽可能多地去除Ca2+。在30℃温育3分钟后,通过加入25%三氯乙酸终止反应,并在Toyo-Roshi膜过滤器(孔径0.45μm)上收集酸可沉淀物质。相同方法测定蛋白激酶C的催化片段,不同之处在于省略了Ca2+,磷脂和二油精。

细胞实验 [1]:

细胞系

B淋巴细胞系

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1nM

应用

12-O-tetradecanoyl phorbol-13-acetate用于活化细胞中的PKC(蛋白激酶C)。

动物实验 [2]:

动物模型

化学皮肤癌变小鼠

剂量

每周处理两次(12.5μg溶于100μL丙酮中)

应用

12-O-tetradecanoyl phorbol-13-acetate用于诱导小鼠皮肤癌

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Castagna M, et al. Direct activation of calcium-activated, phospholipid-dependent protein kinase by tumor-promoting phorbol esters. J Biol Chem. 1982 Jul 10;257(13):7847-51.

[2] Jensen WA, et al. Inhibition of protein kinase C results in decreased expression of bovine leukemia virus. J Virol. 1992 Jul;66(7):4427-33.

[3] Rushworth LK, et al. Dual-specificity phosphatase 5 regulates nuclear ERK activity and suppresses skin cancer by inhibiting mutant Harvey-Ras (HRasQ61L)-driven SerpinB2 expression. Proc Natl Acad Sci U S A. 2014 Dec 23;111(51):18267-72.

质量控制

化学结构

12-O-tetradecanoyl phorbol-13-acetate

相关生物数据

12-O-tetradecanoyl phorbol-13-acetate