生物活性：

Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator^[1][2]. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells

體外研究(In Vitro)：

In order to examine the role of PKC in p38MAPK phosphorylation, the cells are stimulated with the PKC activator, PMA (100 nM), which mimics the binding of DAG, the natural activator of PKC, to the C1 region of the PKCs. p38MAPK phosphorylation by PMA is observed in the two cell types similar to that observed by GnRH in αT3-1 cells, that is, a slow sustained activation (3.2-fold and 3.6-fold, respectively at 30 min). The paradoxical findings that PKCs activated by GnRH and PMA play a differential role in p38MAPK phosphorylation may be explained by differential localization of the PKCs. Basal, GnRH- and PMA- stimulation of p38MAPK phosphorylation in αT3-1 cells is mediated by Ca²⁺ influx via voltage-gated Ca²⁺ channels and Ca²⁺ mobilization, while in the differentiated LβT2 gonadotrope cells it is mediated only by Ca²⁺ mobilization.

THP-1 cells are differentiated into macrophage-like cells (THP-1 macrophages) by incubation in the presence of PMA (200 ng/mL; 1-5 days), which leads to a macrophage-like phenotype characterized by changes in morphology and increased cell surface expression of CD11 and CD14^[3].
In the monocytic cell line THP-1, PMA results in a more differentiated phenotype than VD3, according to adherence, loss of proliferation, phagocytosis of latex beads, and expression of CD11b and CD14

體內(nèi)研究(In Vivo)：

PMA is a PKC agonist, which reverses the damage induced by 5-hydroxydecanoic acid (5-HD). Thus, activation of the mitoKATP protected mitochondrial function in SOD and MDA via the PKC pathway.

溶解性數(shù)據(jù)：

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• 1.

  
  

  請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

  
  

• 2.

  
  

  請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

  
  

• 3.

  
  

  請依序添加每種溶劑： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

  
  

• 4.

  
  

  請依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

  
  

• 5.

  
  

  請依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

  
  

• 6.

  
  

  請依序添加每種溶劑： 10% EtOH    90% corn oil

  Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

參考文獻：

[1]. Sergio E. Alvarez, et al. Autocrine and paracrine roles of sphingosine-1-phosphate. TRENDS in Endocrinology and Metabolism Vol.18 No.8

[2]. Zhang T, et al. MPTP-Induced Depletion in Basolateral Amygdala via Decrease of D2R Activation Suppresses GABAA Receptors Expression and LTD Induction Leading to Anxiety-Like Behaviors. Front Mol Neurosci. 2017 Aug 7;10:247.

[3]. Schwende H, et al. Differences in the state of differentiation of THP-1 cells induced by phorbol ester and 1,25-dihydroxyvitamin D3. J Leukoc Biol. 1996;59(4):555-561.

[4]. Mugami S, et al. Differential roles of PKC isoforms (PKCs) and Ca2+ 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.

[5]. 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;13(3):e0193601. Published 2018 Mar 14.

[6]. Hou S, et al. Mechanism of Mitochondrial Connexin43's Protection of the Neurovascular Unit under Acute Cerebral Ischemia-Reperfusion Injury. Int J Mol Sci. 2016 May 5;17(5). pii: E679.

[7]. Heng-Ching Wen, 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.

Data Sheet

https://file.medchemexpress.cn/batch_PDF/HY-18739/Phorbol-12-myristate-13-acetate-DataSheet-MedChemExpress.pdf