货号:A175370 同义名: 佛波醇12-十四酸酯13-乙酸酯 / PMA;TPA
TPA(佛波酯)通过激活蛋白激酶C(PKC),引发细胞内信号传导途径,导致炎症介质和细胞因子的释放,以及引发氧化应激和免疫细胞激活,最终导致急性接触性皮炎的发生。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
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 | 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 dihydrochloride |
++++
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% | |||||||||||||||||
SIS3 | ✔ | 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 |
98% | |||||||||||||||||
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。 |
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 | 97% | ||||||||||||||||
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。 |
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]. |
Animal study | 急性接触性皮炎/慢性持续性皮肤炎症 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 | 616.825 |
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 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
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 |
动物实验配方 |