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Phorbol 12-myristate 13-acetate

Catalog No. TQ0198   CAS 16561-29-8
Synonyms: PKC, SphK, Nuclear factor-κB, Protein kinase C, Inhibitor, Phorbol 12 myristate 13 acetate, TPA, inhibit, Phorbol 12myristate 13acetate, Phorbol myristate, Nuclear factor-kappaB, Sphingosine kinase, NF-κB, PMA

Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.

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Phorbol 12-myristate 13-acetate, CAS 16561-29-8
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Phorbol 12-myristate 13-acetate (PMA) is a dual SphK and PKC activator.
Targets&IC50 PKC:11.7 nM (EC50)
In vitro p38MAPK phosphorylation by PMA (100 nM) 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 [2].
In vivo PMA 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 [3].
Cell Research αT3-1 and LβT-2 cells are grown in monolayer cultured in DMEM in humidified incubator 5% CO2 at 37°C. Serum starvation is with 0.1% FCS in the same medium for 16 h. GnRH and PMA are then added for the length of time as indicated. In general, αT3-1 cells are transiently transfected by ExGen 500 or by jetPRIME, while LβT2 cells only by jetPRIME transfection reagent. For experiments with dominant-negative (DN) PKCs, αT3-1 cells (in 6 cm plates) are transfected with 1.5 μg of p38α-GFP with 3 μg of control vector, pCDNA3, or with 3 μg of the DN-PKCs constructs. For LβT2 cells, transfections are performed (in 10 cm plates) with 4 μg of p38α-GFP along with 9 μg of control vector, pCDNA3, or with 9 μg of the DN-PKCs constructs. Approximately 30 h after transfection, the cells are serum-starved (0.1% FCS) for 16 h and later stimulated with GnRH or PMA, washed twice with ice-cold PBS, treated with the lysis buffer, followed by one freeze-thaw cycle. Cells are harvested; following centrifugation (15,000×g, 15 min, 4°C) supernatants are taken for immunoprecipitation experiments [2].
Animal Research All experiments are performed with male Wistar rats (weighing 250-280 g). One hundred and thirty-five Wistar rats are randomly divided into seven groups. (1) Rats in the sham group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline; (2) Rats in the IR group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline 30 min before middle cerebral artery occlusion (MCAO); (3) Rats in the Carbenoxolone (CBX) group (n=21) are given a lateral cerebral ventricle injection of CBX (5 μg/mL×10 μL) 30 min before MCAO; (4) Rats in the Sch-6783 group (n=21) are given a lateral cerebral ventricle injection of DZX (2 mM×30 μL) 30 min prior to MCAO; (5) Rats in the 5-HD group (n=21) are given a lateral cerebral ventricle injection of 5-HD (100 mM×10 μL), and after 10 min, DZX is injected 15 min prior to MCAO; (6) The rats in the DZX + Ro group (n=15) are given a lateral cerebral ventricle injection of DZX, and after 10 min, Ro-31-8425 (400 μg/kg) is injected 15 min prior to MCAO; (7) The rats in the 5-HD+PMA group (n=15) are given an intraperitoneal injection of PMA (200 μg/kg) after the injection of 5-HD and DZX [3].
Synonyms PKC, SphK, Nuclear factor-κB, Protein kinase C, Inhibitor, Phorbol 12 myristate 13 acetate, TPA, inhibit, Phorbol 12myristate 13acetate, Phorbol myristate, Nuclear factor-kappaB, Sphingosine kinase, NF-κB, PMA
Molecular Weight 616.836
Formula C36H56O8
CAS No. 16561-29-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (81.06 mM)

H2O: Insoluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Hu H, Jiang H, Zhang K, et al. Memantine nitrate MN-08 suppresses NLRP3 inflammasome activation to protect against sepsis-induced acute lung injury in mice. Biomedicine & Pharmacotherapy. 2022, 156: 113804 1. Sergio E. Alvarez, et al. Autocrine and paracrine roles of sphingosine-1-phosphate. TRENDS in Endocrinology and Metabolism Vol.18 No.8 2. Li Y, Wu Y, Li S, et al. Identification of phytochemicals in Qingfei Paidu decoction for the treatment of coronavirus disease 2019 by targeting the virus-host interactome. Biomedicine & Pharmacotherapy. 2022: 113946. 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. 3 .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.

Related compound libraries

This product is contained In the following compound libraries:
Terpene Natural Product Library GPCR Compound Library TGF-beta/Smad Compound Library Covalent Inhibitor Library Kinase Inhibitor Library Rare Natural Compound Library Neuronal Signaling Compound Library Bioactive Compound Library

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