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Purity: = 99.56%
Phorbol 12-myristate 13-acetate (PMA) is a novel and potent protein kinase C (PKC) agonist with the potential for the treatment of acute myeloid leukemia and cardiac fibrosis. THP-1 cells can differentiate into macrophage-like cells (THP-1 macrophages) in the presence of PMA (200 ng/mL; 1–5 days). A macrophage-like phenotype brought on by PMA is typified by morphological alterations and elevated CD11 and CD14 surface expression.
| Targets |
PKC ( EC50 = 11.7 nM ); NF-κB
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| ln Vitro |
PMA induces Thy-1 up-regulation, raises Thy-1 mRNA and protein levels in endothelial cells, and prevents the formation of capillary-like tubes and endothelial cell migration.[1]
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| ln Vivo |
PMA first increases endothelial cell migration in the zebrafish model, then it activates the PKC-δ/Syk/NF-κB-mediated pathway to up-regulate Thy-1, which in turn prevents endothelial cell migration.[1]
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| Cell Assay |
Monolayer cultured αT3-1 and LβT-2 cells are grown in DMEM in a humidified incubator with 5% CO2 at 37°C. Serum starvation lasts 16 hours when 0.1% FCS is added to the same medium. Then, for the duration specified, GnRH and PMA are added. αT3-1 cells can be transfected temporarily using either jetPRIME or ExGen 500, whereas LβT2 cells can only be transfected using the jetPRIME transfection reagent. In experiments involving dominant-negative (DN) PKCs, 1.5 μg of p38α-GFP or 3 μg of the DN-PKCs constructs are transfected into αT3-1 cells (in 6 cm plates) in combination with pCDNA3, the control vector. Transfections of LβT2 cells are carried out (in 10 cm plates) using 4 μg of p38α-GFP in combination with 9 μg of either the DN-PKCs constructs or the control vector, pCDNA3. The cells are serum starved (0.1% FCS) for 16 hours approximately 30 hours after transfection. They are then stimulated with GnRH or PMA, twice washed with ice-cold PBS, treated with the lysis buffer, and then subjected to one freeze-thaw cycle. After harvesting the cells, the supernatants are taken for immunoprecipitation experiments and centrifuged at 15,000 x g for 15 minutes at 4°C.
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| Animal Protocol |
Rats: Male Wistar rats weighing between 250 and 280 grams are used in all experiments. Seven groups of fifteen thirty-five Wistar rats are randomly assigned. (1) A 0.9% normal saline injection is administered to rats in the sham group (n = 21); (2) A 0.9% normal saline injection is administered to rats in the IR group (n = 21) 30 minutes prior to middle cerebral artery occlusion (MCAO); (3) A lateral cerebral ventricle injection of CBX (5 μg/mL×10 μL) is administered to rats in the Carbenoxolone (CBX) group (n = 21) 30 minutes prior to MCAO; (4) Rats in the Sch-6783 group (n = 21) receive a lateral cerebral ventricle injection of DZX (2 mM×30 μL) 30 minutes before MCAO; (5) Rats in the 5-HD group (n = 21) receive a lateral cerebral ventricle injection of 5-HD (100 mM×10 μL); (6) The rats in the DZX + Ro group (n = 15) receive a lateral cerebral ventricle injection of DZX, and after 10 min, Ro-31-8425 (400 μg/kg) is injected 15 minutes before MCAO; (7) Rats in the 5-HD+PMA group (n = 15) receive an intraperitoneal injection of PMA (200 μg/kg) following the injection of 5-HD and DZX.
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| References |
| Molecular Formula |
C36H56O8
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|---|---|
| Molecular Weight |
616.8251
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| Exact Mass |
616.4
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| Elemental Analysis |
C, 70.10; H, 9.15; O, 20.75
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| CAS # |
16561-29-8
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| Appearance |
Solid powder
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| SMILES |
CCCCCCCCCCCCCC(=O)O[C@@H]1[C@H]([C@]2([C@@H](C=C(C[C@]3([C@H]2C=C(C3=O)C)O)CO)[C@H]4[C@@]1(C4(C)C)OC(=O)C)O)C
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| InChi Key |
PHEDXBVPIONUQT-RGYGYFBISA-N
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| InChi Code |
InChI=1S/C36H56O8/c1-7-8-9-10-11-12-13-14-15-16-17-18-29(39)43-32-24(3)35(42)27(30-33(5,6)36(30,32)44-25(4)38)20-26(22-37)21-34(41)28(35)19-23(2)31(34)40/h19-20,24,27-28,30,32,37,41-42H,7-18,21-22H2,1-6H3/t24-,27+,28-,30-,32-,34-,35-,36-/m1/s1
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| Chemical Name |
[(1S,2S,6R,10S,11R,13S,14R,15R)-13-acetyloxy-1,6-dihydroxy-8-(hydroxymethyl)-4,12,12,15-tetramethyl-5-oxo-14-tetracyclo[8.5.0.02,6.011,13]pentadeca-3,8-dienyl] tetradecanoate
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| Synonyms |
NSC262244; PD616; NSC 262244; NSC-262244; PD-616; RP-323; PD 616; RP 323; PMA; RP323
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~162.1 mM)
Ethanol: ~100 mg/mL (~162.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.05 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 2.5 mg/mL (4.05 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (4.05 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 5%DMSO + Corn oil: 5.0mg/ml (8.11mM) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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