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Phorbol 12-myristate 13-acetate/佛波酯 {[allProObj[0].p_purity_real_show]}

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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Phorbol 12-myristate 13-acetate/佛波酯 化学结构 CAS号:16561-29-8
Phorbol 12-myristate 13-acetate/佛波酯 化学结构
CAS号:16561-29-8
Phorbol 12-myristate 13-acetate/佛波酯 3D分子结构
CAS号:16561-29-8
Phorbol 12-myristate 13-acetate/佛波酯 化学结构 CAS号:16561-29-8
Phorbol 12-myristate 13-acetate/佛波酯 3D分子结构 CAS号:16561-29-8
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Phorbol 12-myristate 13-acetate/佛波酯 纯度/质量文件 产品仅供科研

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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。

Phorbol 12-myristate 13-acetate/佛波酯 生物活性

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].

Phorbol 12-myristate 13-acetate/佛波酯 细胞实验

Cell Line
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.

Phorbol 12-myristate 13-acetate/佛波酯 动物实验

Species
Animal Model
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

Phorbol 12-myristate 13-acetate/佛波酯 动物研究

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。

Phorbol 12-myristate 13-acetate/佛波酯 临床研究

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 <<

Phorbol 12-myristate 13-acetate/佛波酯 参考文献

[1]Mugami S, Kravchook S, et al. Differential roles of PKC isoforms (PKCs) and Ca(2+) 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.

[2]Xu F, Satoh E, et al. Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4. Br J Pharmacol. 2003 Sep;140(2):413-21. Epub 2003 Aug 11.

[3]Blumberg PM. Protein kinase C as the receptor for the phorbol ester tumor promoters: sixth Rhoads memorial award lecture. Cancer Res. 1988 Jan 1;48(1):1-8.

[4]Kawasaki H, Springett GM, Toki S, Canales JJ, Harlan P, Blumenstiel JP, Chen EJ, Bany IA, Mochizuki N, Ashbacher A, Matsuda M, Housman DE, Graybiel AM. A Rap guanine nucleotide exchange factor enriched highly in the basal ganglia. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13278-83.

[5]Jiang Y, Fleet JC. Effect of phorbol 12-myristate 13-acetate activated signaling pathways on 1α, 25 dihydroxyvitamin D3 regulated human 25-hydroxyvitamin D3 24-hydroxylase gene expression in differentiated Caco-2 cells. J Cell Biochem. 2012 May;113(5):1599-607.

[6]Gordon JR, Galli SJ. Phorbol 12-myristate 13-acetate-induced development of functionally active mast cells in W/Wv but not Sl/Sld genetically mast cell-deficient mice. Blood. 1990 Apr 15;75(8):1637-45.

[7]Hurley JH, Newton AC, Parker PJ, Blumberg PM, Nishizuka Y. Taxonomy and function of C1 protein kinase C homology domains. Protein Sci. 1997 Feb;6(2):477-80.

[8]De Vry CG, Valdez M, Lazarov M, et al. Topical application of a novel immunomodulatory peptide, RDP58, reduces skin inflammation in the phorbol ester-induced dermatitis model. J Invest Dermatol. 2005;125(3):473-481.

Phorbol 12-myristate 13-acetate/佛波酯 实验方案

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

Phorbol 12-myristate 13-acetate/佛波酯 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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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