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Phorbol 12-myristate 13-acetate [16561-29-8]

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Cat# HY-18739-10mg

Size : 10mg

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Phone : +1 850 650 7790

Brand : MedChemExpress

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Description

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^[3]^[7].

IC₅₀ & Target^[1]^[7]

PKC

11.7 nM (EC₅₀)

NF-κB

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	EC₅₀	0.7 nM Compound: 13	Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
MT4	EC₅₀	0.9 nM Compound: 13	Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay	[PMID: 25970561]
SNU-387	IC₅₀	> 10 μM Compound: 10	Cytotoxicity against human SNU387 cells after 48 hrs by MTT assay Cytotoxicity against human SNU387 cells after 48 hrs by MTT assay	[PMID: 23701597]
U-937	EC₅₀	0.45 nM Compound: PMA	Induction of attachment of U937 cells after 48 hrs Induction of attachment of U937 cells after 48 hrs	[PMID: 17284021]
Vero	EC₅₀	> 162 μM Compound: 4, TPA	Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay	[PMID: 23215460]
Vero	EC₅₀	0.0029 μM Compound: 4, TPA	Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay	[PMID: 23215460]
Vero	EC₅₀	2.2 μM Compound: 4, TPA	Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay	[PMID: 23215460]
Vero	EC₅₀	2.9 nM Compound: 13	Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days	[PMID: 25970561]
Vero	CC₅₀	5.7 μM Compound: 4, TPA	Cytotoxicity against african green monkey Vero cells by MTS assay Cytotoxicity against african green monkey Vero cells by MTS assay	[PMID: 23215460]
Vero	CC₅₀	5.7 μM Compound: TPA	Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method	[PMID: 28925702]

In Vitro

PMA (100, 200 ng/mL; 1-5 days) induce THP-1 cells to differentiate into macrophage-like cells (THP-1 macrophages), characterized by changes in morphology (adherent macrophage-like phenotype), and increases cell surface expression of CD11b^[3]^[5].
PMA (20 ng/mL, 36 h) inhibits endothelial cell migration through activating the PKC-δ/Syk/NF-κB-mediated up-regulation of Thy-1^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (162.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (162.12 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6212 mL	8.1060 mL	16.2119 mL
5 mM	0.3242 mL	1.6212 mL	3.2424 mL
10 mM	0.1621 mL	0.8106 mL	1.6212 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.80%

Data Sheet (286 KB) SDS (746 KB)

COA (247 KB) HNMR (164 KB) RP-HPLC (163 KB) LCMS (385 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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Phorbol 12-myristate 13-acetate [16561-29-8]

Cat# HY-18739-10mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

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