Phorbol 12-myristate 13-acetate
Chemical Name: (1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-(Acetyloxy)-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1H-cyclopropa[3,4]benz[1,2-e]azulen-9-yl tetradecanoate
Purity: ≥98%
Biological Activity
Phorbol 12-myristate 13-acetate is an extensively used phorbol ester high affinity activator of protein kinase C (Ki = 2.6 nM as measured by displacement of [3H]phorbol 12,13-dibutyrate binding in rat cortex synaptosomal membranes). It binds to the C1a and C1b domains of PKC inducing membrane translocation of PKC. Phorbol 12-myristate 13-acetate activates the PKC isoforms PKCα, -β, -γ, -δ, -ε, -η, and -θ but not PKCζ or -ι/λ. Phorbol 12-myristate 13-acetate is a tumor promoter. Phorbol 12-myristate 13-acetate can also induce differentiation of THP-1 monocytes to a macrophage phenotype in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Direct activation of calcium-activated, phospholipid-dependent protein kinase by tumor-promoting phorbol esters.
Castagna et al.
J.Biol.Chem., 1982;257:7847 -
A diacylglycerol analogue reduces neuronal calcium currents independently of protein kinase C activation.
Hockberger et al.
Nature, 1989;338:340 -
Structural determinants of phorbol ester binding in synaptosomes: pharmacokinetics and pharmacodynamics.
Murphy et al.
Eur.J.Pharmacol., 1999;381:77
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Citations for Phorbol 12-myristate 13-acetate
The citations listed below are publications that use Tocris products. Selected citations for Phorbol 12-myristate 13-acetate include:
28 Citations: Showing 1 - 10
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Manipulation of Gut Microbiota Influences Immune Responses, Axon Preservation, and Motor Disability in a Model of Progressive Multiple Sclerosis.
Authors: Mestre Et al.
Front Immunol 2019;10:1374
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Developmental protein kinase C hyper-activation results in microcephaly and behavioral abnormalities in zebrafish.
Authors: Liu Et al.
Transl Psychiatry 2018;8:232
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Hypertension-evoked RhoA activity in vascular smooth muscle cells requires RGS5.
Authors: Arnold Et al.
FASEB J 2018;32:2021
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PKCε Inhibits Neuronal Dendritic Spine Development through Dual Phosphorylation of Ephexin5.
Authors: Schaffer Et al.
Cell Rep 2018;25:2470
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Molecular mechanism: the human DA transporter histidine 547 regulates basal and HIV-1 Tatprotein-inhibited DA transport.
Authors: Quizon
Scientific Reports 2016;6:39048
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A High Throughput Phenotypic Screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells.
Authors: Cicero Et al.
Sci Rep 2016;6:34798
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New functional activity of aripipr. revealed: Robust antagonism of D2 DA receptor-stimulated Gβγ signaling.
Authors: Brust Et al.
J Vis Exp 2015;93:85
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Comparative Multi-Donor Study of IFNγ Secretion and Expression by Human PBMCs Using ELISPOT Side-by-Side with ELISA and Flow Cytometry Assays.
Authors: Hagen Et al.
Cells 2015;4:84
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Levitational Image Cytometry with Temporal Resolution.
Authors: Tasoglu Et al.
Adv Mater 2015;27:3901
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The ATP-Binding Cassette Transporter-2 (ABCA2) Overexpression Modulates Sphingosine Levels and Transcription of the Amyloid Precursor Protein (APP) Gene.
Authors: Davis
Biochem Pharmacol 2015;12:847
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Autism-associated mutation inhibits protein kinase C-mediated neuroligin-4X enhancement of excitatory synapses.
Authors: Bemben Et al.
Proc Natl Acad Sci U S A 2015;112:2551
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Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis.
Authors: Brown Et al.
J Pharmacol Exp Ther 2014;88:13149
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Transactivation of epidermal growth factor receptor through platelet-activating factor/receptor in ovarian cancer cells.
Authors: Yu Et al.
J Exp Clin Cancer Res 2014;33:85
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The role of Nox1 and Nox2 in GPVI-dependent platelet activation and thrombus formation.
Authors: Walsh Et al.
Redox Biol 2014;2:178
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PMA induces SnoN proteolysis and CD61 expression through an autocrine mechanism.
Authors: Li Et al.
Cell Signal 2014;26:1369
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Heteromeric MT1/MT2 melatonin receptors modulate photoreceptor function.
Authors: Baba Et al.
Sci Signal 2013;6:ra89
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The analysis of purkinje cell dendritic morphology in organotypic slice cultures.
Authors: Kapfhammer and Gugger
J Biol Chem 2012;NULL
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Transient receptor potential vanilloid type 1-dependent regulation of liver-related neurons in the paraventricular nucleus of the hypothalamus diminished in the type 1 diabetic mouse.
Authors: Gao Et al.
J Virol 2012;61:1381
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Small molecule positive allosteric modulation of TRPV1 activation by vanilloids and acidic pH.
Authors: Kaszás Et al.
J Neurosci 2012;340:152
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Glucose-mediated control of ghrelin release from primary cultures of gastric mucosal cells.
Authors: Sakata Et al.
Am J Physiol Endocrinol Metab 2012;302:E1300
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The acid-sensitive, anesthetic-activated potassium leak channel, KCNK3, is regulated by 14-3-3β-dependent, protein kinase C (PKC)-mediated endocytic trafficking.
Authors: Gabriel Et al.
J Biol Chem 2012;287:32354
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Functional plasticity of central TRPV1 receptors in brainstem dorsal vagal complex circuits of streptozotocin-treated hyperglycemic mice.
Authors: Zsombok Et al.
Curr Alzheimer Res 2011;31:14024
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The plasma membrane-associated GTPase Rin interacts with the DA transporter and is required for protein kinase C-regulated DA transporter trafficking.
Authors: Navaroli Et al.
J Neurosci 2011;31:13758
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Regulation of glycine receptor diffusion properties and gephyrin interactions by protein kinase C.
Authors: Specht Et al.
EMBO J 2011;30:3842
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Involvement of the chemokine-like receptor GPR33 in innate immunity.
Authors: Bohnekamp Et al.
Br J Pharmacol 2010;396:272
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Inhibition of ATR protein kinase activity by schisandrin B in DNA damage response.
Authors: Nishida Et al.
Nucleic Acids Res 2009;37:5678
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Regulation of SHP-1 tyrosine phosphatase in human platelets by serine phosphorylation at its C terminus.
Authors: Jones Et al.
Biochem Biophys Res Commun 2004;279:40475
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Nifedipine facilitates neurotransmitter release independently of calcium channels.
Authors: Hirasawa
Proc Natl Acad Sci U S A 2003;100:6139
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