货号:A175370
                
                同义名:
                    
                        
                            佛波醇12-十四酸酯13-乙酸酯
                            
                             / PMA; TPA
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
Phorbol 12-myristate 13-acetate是一种PKC激活的佛波酯类化合物,能够剂量依赖性地提高细胞内钙离子浓度,其EC50为11.7nM。PMA可以用于激活PKC从而激活NETosis的发生。Phorbol 12-myristate 13-acetate刺激间充质干细胞的心脏分化,促进造血分化。
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| Type | HazMat fee for 500 gram (Estimated) | 
| Excepted Quantity | USD 0.00 | 
| Limited Quantity | USD 15-60 | 
| Inaccessible (Haz class 6.1), Domestic | USD 80+ | 
| Inaccessible (Haz class 6.1), International | USD 150+ | 
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ | 
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ | 
 
                                 
                                
                            

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| 产品名称 | PKC ↓ ↑ | PKCα ↓ ↑ | PKCβ ↓ ↑ | PKCγ ↓ ↑ | PKCδ ↓ ↑ | PKCε ↓ ↑ | PKCζ ↓ ↑ | PKCη ↓ ↑ | PKCθ ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Daphnetin | + PKC, IC50: 25.01 μM | PKA,EGFR | 95% | ||||||||||||||||
| Dequalinium Chloride | 99%+ | ||||||||||||||||||
| Quercetin | ✔ | Sirtuin,Src | 95% | ||||||||||||||||
| Myricetrin | ✔ | 96% | |||||||||||||||||
| Go 6983 | +++ PKCα, IC50: 7 nM | +++ PKCβ, IC50: 7 nM | +++ PKCγ, IC50: 6 nM | +++ PKCδ, IC50: 10 nM | ++ PKCζ, IC50: 60 nM | 99%+ | |||||||||||||
| Go6976 | +++ PKC, IC50: 7.9 nM | ++++ PKCα, IC50: 2.3 nM | +++ PKCβ1, IC50: 6.2 nM | FLT3 | 99%+ | ||||||||||||||
| Bisindolylmaleimide I | +++ PKCα, IC50: 20 nM | +++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM | +++ PKCγ, IC50: 20 nM | 99%+ | |||||||||||||||
| Lawsone methyl ether | ✔ | 99% | |||||||||||||||||
| Sotrastaurin | ++++ PKCα, Ki: 0.95 nM | ++++ PKCβ1, Ki: 0.64 nM | ++++ PKCδ, Ki: 2.1 nM | ++++ PKCε, Ki: 3.2 nM | ++++ PKCη, Ki: 1.8 nM | ++++ PKCθ, Ki: 0.22 nM | 99%+ | ||||||||||||
| Enzastaurin | ++ PKCα, IC50: 39 nM | +++ PKCβ, IC50: 6 nM | + PKCγ, IC50: 83 nM | + PKCε, IC50: 110 nM | 98% | ||||||||||||||
| Midostaurin | ++ PKCα, IC50: 22 nM | ++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM | ++ PKCγ, IC50: 24 nM | + PKCδ, IC50: 330 nM | + PKCε, IC50: 1.25 μM | + PKCη, IC50: 160 nM | 99% | ||||||||||||
| Ro 31-8220 mesylate | ++++ PKCα, IC50: 5 nM | +++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM | ++ PKCγ, IC50: 27 nM | ++ PKCε, IC50: 24 nM | 99%+ | ||||||||||||||
| Staurosporine | ++++ PKCα, IC50: 2 nM | ++++ PKCγ, IC50: 5 nM | +++ PKCδ, IC50: 20 nM | ++ PKCε, IC50: 73 nM | ++++ PKCη, IC50: 4 nM | 99%+ | |||||||||||||
| Ruboxistaurin HCl | + PKCα, IC50: 0.36 μM | ++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM | + PKCγ, IC50: 0.3 μM | + PKCδ, IC50: 0.25 μM | ++ PKCη, IC50: 0.052 μM | 99%+ | |||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LDN193189 | ++++ ALK1, IC50: 0.8 nM | ++++ ALK2, IC50: 0.8 nM | +++ ALK3, IC50: 5.3 nM | +++ ALK6, IC50: 16.7 nM | 99%+ | ||||||||||||||
| LDN-212854 | ++++ ALK1, IC50: 2.4 nM | ++++ ALK2, IC50: 1.3 nM | + ALK3, IC50: 85.8 nM | + ALK4, IC50: 2133 nM | + ALK5, IC50: 9276 nM | 99%+ | |||||||||||||
| ML347 | ++ ALK1, IC50: 46 nM | ++ ALK2, IC50: 32 nM | 98% | ||||||||||||||||
| K02288 | ++++ ALK1, IC50: 1.8 nM | ++++ ALK2, IC50: 1.1 nM | ++ ALK3, IC50: 34.4 nM | +++ ALK6, IC50: 6.4 nM | 99%+ | ||||||||||||||
| LDN-193189 2HCl | ++++ ALK1, IC50: 0.8 nM | ++++ ALK2, IC50: 0.8 nM | +++ ALK3, IC50: 5.3 nM | +++ ALK6, IC50: 16.7 nM | 99% | ||||||||||||||
| LDN-214117 | ++ ALK2, IC50: 24 nM | 98% | |||||||||||||||||
| DMH-1 | + ALK2, IC50: 107.9 nM | 99%+ | |||||||||||||||||
| SB-505124 | + ALK4, IC50: 129 nM | ++ ALK5, IC50: 47 nM | 99%+ | ||||||||||||||||
| Vactosertib | +++ ALK4, IC50: 13 nM | +++ ALK5, IC50: 11 nM | 99%+ | ||||||||||||||||
| Alantolactone | ✔ | 98% | |||||||||||||||||
| (E/Z)-SIS3 free base | ✔ | 97% | |||||||||||||||||
| Pirfenidone | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| RepSox | ++++ TGFβR1(ALK5), IC50: 4 nM | 98% | |||||||||||||||||
| GW788388 | +++ ALK5, IC50: 18 nM | 98% | |||||||||||||||||
| LY364947 | ++ TGFβRI, IC50: 59 nM | + TGFβRII, IC50: 0.4 μM | 98% | ||||||||||||||||
| SD-208 | ++ TGF-βRI (ALK5), IC50: 48 nM | 99% | |||||||||||||||||
| SB-525334 | +++ TGFβR1(ALK5), IC50: 14.3 nM | 99%+ | |||||||||||||||||
| LY2109761 | ++ TβRI, Ki: 38 nM | + TβRII, Ki: 300 nM | 99%+ | ||||||||||||||||
| Galunisertib | ++ TβRI, IC50: 56 nM | 98% | |||||||||||||||||
| SB 431542 | + ALK5, IC50: 94 nM | 99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Protein kinase C (PKC) is a key molecule involved in cell growth, apoptosis, and differentiation. Phorbol 12-Myristate 13-Acetate (PMA) is an activator of certain types of PKC, including group A and group B isoforms[3]. Stimulation with 1 μM PMA for 3 min resulted in promoted nucleotide exchange activity in 293T cells[4]. In differentiated Caco-2 cells, pretreatment with 100 nM PMA for 5 min followed by 2h incubation with 10 nM 1,25(OH)2D3 resulted in a 2.6-fold increase in hCYP24A1 mRNA level compared to cells treated by 1,25(OH)2D3 alone. Incubation with 100 nM PMA for 30 min resulted in the activation of ERK1/2 and p38 kinase in Caco-2 cells, whereas pretreatment with the MEK inhibitor U0126 at 10, 20 or 100 μM completely inhibited ERK1/2 activation by PMA and partially suppressed PMA-induced p38 kinase activation. Cells pre-treated with 10 μM U0126 or 8 μM p38 kinase inhibitor SB202190 showed reduced enhancing effect of PMA on 1,25(OH)2D3-induced hCYP24A1 promoter activity[5]. In both W/Wv genetically mast cell-deficient mice and congenic normal mice, repeated administration of PMA (5 μg, 3 times per week for 6 weeks) to the ear skin remarkably increased the number of dermal mast cells[6]. | 
| Concentration | Treated Time | Description | References | |
| NK cells | 50 ng/ml | 4 h | To evaluate NK cell activation by measuring granzyme B production. | Front Immunol. 2019 Jun 27;10:1467. | 
| THP-1 cells | 100 ng/mL | 24 hours | Induced THP-1 cells to differentiate into macrophages for subsequent experiments | Acta Pharm Sin B. 2021 Nov;11(11):3493-3507. | 
| THP-1 cells | 100 ng/ml PMA | 48 hours | Differentiate THP-1 cells into macrophages | Nat Microbiol. 2020 Sep;5(9):1088-1095 | 
| U937 cells | 1 ng/mL | 48 hours | To investigate the effect of monocyte differentiation into macrophages on KYN pathway activation. Results showed significant induction of IDO1 mRNA expression, suggesting that differentiation of monocytes into macrophages may promote KYN pathway activation. | Respir Res. 2024 Jan 14;25(1):31 | 
| THP1 cells | 10 ng/mL | 48 hours | To investigate the effect of monocyte differentiation into macrophages on KYN pathway activation. Results showed significant induction of IDO1 mRNA expression, suggesting that differentiation of monocytes into macrophages may promote KYN pathway activation. | Respir Res. 2024 Jan 14;25(1):31 | 
| THP-1 cells | 100 ng/mL | 48 hours | THP-1 cells were stimulated with PMA to differentiate into macrophages for the preparation of conditioned media. | Neoplasia. 2021 Jun;23(6):561-573 | 
| THP-1 cells | 160 nM PMA and 100 ng/ml LPS | 48 hours | Assess the anti-inflammatory capacity of the coating, results showed PEI/TIR/GS/OxHA significantly inhibited monocyte activation and intracellular ROS generation. | Bioact Mater. 2025 Feb 26;48:443-457 | 
| THP-1 cells | 100 ng/mL PMA | 48 hours | Differentiate THP-1 cells into macrophages for subsequent experiments. | J Exp Clin Cancer Res. 2024 Dec 26;43(1):332 | 
| Raw264.7 cells | 200 nM | 72 hours | To study the effect of VUF11207 on macrophage-like cells, results showed that VUF11207 reversed GAM-induced immunosuppression. | Cell Death Dis. 2024 Jun 19;15(6):434 | 
| THP-1 cells | 200 nM | 72 hours | To study the effect of VUF11207 on macrophage-like cells, results showed that VUF11207 reversed GAM-induced immunosuppression. | Cell Death Dis. 2024 Jun 19;15(6):434 | 
| UACC903 cells | 10 nM | 6 hours | TPA increased the expression and kinase activity of CK1ε and CK1δ. | Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. | 
| HEK293T cells | 10 nM | 6 hours | TPA enhanced CK1ε-mediated Wnt signaling activation and increased cytosolic β-catenin levels. | Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. | 
| MEG-01 cells | 20 nM PMA | 2 days | To study the role of DUSP4 in MEG-01 cell differentiation, it was found that DUSP4 mRNA and protein levels positively correlated with megakaryocyte differentiation. | Cell Rep. 2021 Jul 27;36(4):109421. | 
| THP-1 cells | 100 nM | 48-72 hours | To induce THP-1 cell differentiation into M0 macrophages and further into TAMs to mimic the HCC tumor microenvironment. | J Immunother Cancer. 2022 Dec;10(12):e005655. | 
| U937 cells | 10 ng/mL | Induction of U937 cells into tumor-associated macrophages (TAMs) | Theranostics. 2018 Apr 30;8(11):3074-3086. | |
| T-cells | 5 ng/mL | 16 h | Activate T-cells for studying their interaction with dendritic cells | Front Immunol. 2019 Mar 12;10:448. | 
| CD4+Foxp3+Treg cells | 50 ng/mL | 4 h | stimulation for intracellular cytokine staining | Immunity. 2012 Sep 21;37(3):501-10. | 
| B cells | 50 ng/ml | 4 h | To detect IL-6 and IL-10 expression in B cells, results showed that JDM patient B cells produced less IL-10 after TLR7 activation, while IL-6 expression was similar to healthy controls. | Front Immunol. 2018 Jun 22;9:1372. | 
| Mouse skin cells | 50 ng/mL | 48 h | To evaluate the effect of PMA on IL-1β production in mouse skin cells. Results showed that PMA treatment significantly increased IL-1β production. | PLoS Pathog. 2017 Feb 13;13(2):e1006196. | 
| 3A9 T cells | 100 nM | 6 h | Used for T cell polarization experiments to observe T cell differentiation and cytokine production | J Exp Med. 2003 Apr 7;197(7):899-906. | 
| NK cells | 50 ng/ml | 2 h | To evaluate NK cell activation by measuring IFN-γ and granzyme B production. | Front Immunol. 2019 Jun 27;10:1467. | 
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Irritant contact dermatitis | Topical administration | 0.08 μM | Single dose, imaging after 6 hours | To validate the specificity of PMA in inducing inflammation, results showed increased fluorescence signal in the PMA-treated hindpaw of wildtype mice, while no fluorescence signal was detected in MPO-KO mice. | Theranostics. 2019 Oct 12;9(25):7525-7536 | 
| Animal study | 急性接触性皮炎/慢性持续性皮肤炎症[8] 动物:FVB/N小鼠,雌性,6~8周龄。 给药:将浓度0.03% (wt/v,溶于丙酮),10 μL的TPA单次涂抹于双耳内外表面。 | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT01195272 | Rheumatoid Arthritis | Phase 4 | Completed | - | United Kingdom ... 展开 >> Liverpool, United Kingdom, L9 7AL 收起 << | 
| NCT01195272 | - | Completed | - | - | |
| NCT02137876 | - | Withdrawn(Subject recruitment ... 展开 >>was unsuccessful.) 收起 << | - | United States, Illinois ... 展开 >> Northwestern University Comprehensive Transplant Center Chicago, Illinois, United States, 60611 收起 << | |
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.62mL 0.32mL 0.16mL | 8.11mL 1.62mL 0.81mL | 16.21mL 3.24mL 1.62mL | |
| CAS号 | 16561-29-8 | 
| 分子式 | C36H56O8 | 
| 分子量 | 616.83 | 
| SMILES Code | CCCCCCCCCCCCCC(O[C@H]([C@H]1C)[C@]2(OC(C)=O)[C@@]([C@@](C=C(CO)C[C@]34O)([H])[C@@]1(O)[C@]4([H])C=C(C)C3=O)([H])C2(C)C)=O | 
| MDL No. | MFCD00036736 | 
| 别名 | 佛波醇12-十四酸酯13-乙酸酯 ;PMA; TPA; Phorbol myristate acetate; RP-323; PD-616; NSC-262244; 12-O-Tetradecanoylphorbol-13-acetate | 
| 运输 | 蓝冰 | 
| InChI Key | PHEDXBVPIONUQT-RGYGYFBISA-N | 
| Pubchem ID | 27924 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C | 
| 溶解方案 | DMSO: 105 mg/mL(170.23 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 100 mg/mL(162.12 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
 
 
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