12-O-tetradecanoyl phorbol-13-acetate (PMA)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
12-O-tetradecanoyl phorbol-13-acetate（TPA）是ERK/MAPK的激活剂，有效浓度为50 μM[1]。
ERK是一种胞外信号调节激酶，可与MAPK协作，将信号由细胞表面的受体传导至DNA。据报道，ERK缺陷可导致细胞生长不受控制，被视为治愈癌症的靶标。
TPA是一种强效的ERK激活剂。在A549细胞（人类肺癌细胞系）中，TPA可引起早发、强烈且相对短暂的ERK磷酸化[2]。在小鼠DUSP5（+/+）胚胎纤维母细胞中， TPA可增加ERK表达水平[3]。
在表达ERK荧光共振能量转移（FRET）生物传感器的转基因（Eisuke）小鼠中，TPA 处理使ERK活性逐步提升，并在约6 hr后达到峰值[1]。
也有报道表示，在S100A9转基因小鼠中，在表皮癌变（对肿瘤形成重要）期间，TPA处理可增加不成熟骨髓细胞的积累和乳头状瘤的形成[4]。
参考文献：
[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.
- 1. Yi Zhang, Feifei Luo, et al. "Soluble NKG2D Ligands Impair CD8+ T Cell Anti-Tumor Function Dependent Of NKG2D Downregulation In The Neuroblastoma." Research Square. February 25th, 2022.
- 2. Li Yuan, Lingming Zhang, et al. "Upregulation of UGT1A1 expression by ursolic acid and oleanolic acid via the inhibition of the PKC/NF-κB signaling pathway." Phytomedicine. 2021 Nov;92:153726. PMID: 34536821
- 3. Mengfei Zhang, Na Li, et al. "Eif2s3y Promotes the Proliferation of Spermatogonial Stem Cells by Activating ERK Signaling." Stem Cells Int. 2021 Jan 29;2021:6668658. PMID: 33603791
- 4. 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
| Storage | Store at -20°C |
| M.Wt | 616.83 |
| Cas No. | 16561-29-8 |
| Formula | C36H56O8 |
| Solubility | insoluble in H2O; ≥112.9 mg/mL in DMSO; ≥80 mg/mL in EtOH |
| Chemical Name | (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-acetoxy-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-1H-cyclopropa[3,4]benzo[1,2-e]azulen-9-yl tetradecanoate |
| SDF | Download SDF |
| Canonical SMILES | CCCCCCCCCCCCCC(O[C@@H]1[C@@H](C)[C@@]([C@H](C=C(C)C2=O)[C@]2(O)CC(CO)=C3)(O)[C@@H]3[C@H]4[C@]1(OC(C)=O)C4(C)C)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 酶学实验 [1]: | |
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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]: | |
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细胞系 |
B淋巴细胞系 |
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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。 |
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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]: | |
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动物模型 |
化学皮肤癌变小鼠 |
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剂量 |
每周处理两次（12.5μg溶于100μL丙酮中） |
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应用 |
12-O-tetradecanoyl phorbol-13-acetate用于诱导小鼠皮肤癌 |
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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。 |
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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. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
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