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Phorbol 12-myristate 13-acetate

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Chemical Structure| 16561-29-8 同义名 : 佛波醇12-十四酸酯13-乙酸酯 ;PMA;TPA;Phorbol myristate acetate;RP-323;PD-616;NSC-262244;12-O-Tetradecanoylphorbol-13-acetate
CAS号 : 16561-29-8
货号 : A175370
分子式 : C36H56O8
纯度 : 95%
分子量 : 616.825
MDL号 : MFCD00036736
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(170.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(162.12 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
描述 Protein kinase C (PKC) is a key molecule involved in cell growth, apoptosis, and differentiation. Phorbol 12-Myristate 13-Acetate (PMA) is an activator of certain types of PKC, including group A and group B isoforms[3]. Stimulation with 1 μM PMA for 3 min resulted in promoted nucleotide exchange activity in 293T cells[4]. In differentiated Caco-2 cells, pretreatment with 100 nM PMA for 5 min followed by 2h incubation with 10 nM 1,25(OH)2D3 resulted in a 2.6-fold increase in hCYP24A1 mRNA level compared to cells treated by 1,25(OH)2D3 alone. Incubation with 100 nM PMA for 30 min resulted in the activation of ERK1/2 and p38 kinase in Caco-2 cells, whereas pretreatment with the MEK inhibitor U0126 at 10, 20 or 100 μM completely inhibited ERK1/2 activation by PMA and partially suppressed PMA-induced p38 kinase activation. Cells pre-treated with 10 μM U0126 or 8 μM p38 kinase inhibitor SB202190 showed reduced enhancing effect of PMA on 1,25(OH)2D3-induced hCYP24A1 promoter activity[5]. In both W/Wv genetically mast cell-deficient mice and congenic normal mice, repeated administration of PMA (5 μg, 3 times per week for 6 weeks) to the ear skin remarkably increased the number of dermal mast cells[6].
作用机制 PMA is a phorbol ester structurally analogous to diacylglycerol. It activates PKC isoforms by associating with their C1 domains[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01195272 Rheumatoid Arthritis Phase 4 Completed - United Kingdom ... 展开 >> Liverpool, United Kingdom, L9 7AL 收起 <<
NCT01195272 - Completed - -
NCT02137876 - Withdrawn(Subject recruitment ... 展开 >>was unsuccessful.) 收起 << - United States, Illinois ... 展开 >> Northwestern University Comprehensive Transplant Center Chicago, Illinois, United States, 60611 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.11mL

1.62mL

0.81mL

16.21mL

3.24mL

1.62mL
参考文献

[1]Mugami S, Kravchook S, et al. Differential roles of PKC isoforms (PKCs) and Ca(2+) in GnRH and phorbol 12-myristate 13-acetate(PMA) stimulation of p38MAPK phosphorylation in immortalized gonadotrope cells. Mol Cell Endocrinol. 2017 Jan 5;439:141-154.

[2]Xu F, Satoh E, et al. Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4. Br J Pharmacol. 2003 Sep;140(2):413-21. Epub 2003 Aug 11.

[3]Blumberg PM. Protein kinase C as the receptor for the phorbol ester tumor promoters: sixth Rhoads memorial award lecture. Cancer Res. 1988 Jan 1;48(1):1-8.

[4]Kawasaki H, Springett GM, Toki S, Canales JJ, Harlan P, Blumenstiel JP, Chen EJ, Bany IA, Mochizuki N, Ashbacher A, Matsuda M, Housman DE, Graybiel AM. A Rap guanine nucleotide exchange factor enriched highly in the basal ganglia. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13278-83.

[5]Jiang Y, Fleet JC. Effect of phorbol 12-myristate 13-acetate activated signaling pathways on 1α, 25 dihydroxyvitamin D3 regulated human 25-hydroxyvitamin D3 24-hydroxylase gene expression in differentiated Caco-2 cells. J Cell Biochem. 2012 May;113(5):1599-607.

[6]Gordon JR, Galli SJ. Phorbol 12-myristate 13-acetate-induced development of functionally active mast cells in W/Wv but not Sl/Sld genetically mast cell-deficient mice. Blood. 1990 Apr 15;75(8):1637-45.

[7]Hurley JH, Newton AC, Parker PJ, Blumberg PM, Nishizuka Y. Taxonomy and function of C1 protein kinase C homology domains. Protein Sci. 1997 Feb;6(2):477-80.