ERK/MAPK 激活劑 -12-O-tetradecanoyl phorbol-13-acetate (TPA)

12-O-tetradecanoyl phorbol-13-acetate (PMA) CAS#16561-29-8 APExBIO貨號N2060

(Synonyms: PMA; TPA; Phorbol myristate acetate)

12-O-tetradecanoyl phorbol-13-acetate (TPA) 是 ERK/MAPK 的激活劑，濃度為 50μm [1]。ERK 是一種細胞外信號調節激酶，與 MAPK 協同將信號從細胞表面的受體轉移到 DNA。據報導，ERK 缺乏會導致細胞不受控制地生長，並被視為治愈癌症的靶點。12-O-tetradecanoyl phorbol-13-acetate (TPA) 是一種有效的 ERK 激活劑。當用 A549 細胞（人肺癌細胞系）進行測試時，12-O-tetradecanoyl phorbol-13-acetate (TPA) 處理導致早期、強烈且相對短暫的 ERK 磷酸化 [2]。在來自 DUSP5 (+/+) 小鼠的小鼠胚胎成纖維細胞中，12-O-tetradecanoyl phorbol-13-acetate (TPA) 的施用增加了 ERK 表達水平 [3]。在表達 ERK 的第一共振能量轉移 (FRET) 生物傳感器的轉基因 (Eisuke) 小鼠中，ERK 活性在局部12-O-tetradecanoyl phorbol-13-acetate (TPA) 治療後逐漸受到刺激，並在大約 6 小時後達到峰值 [1]。另據報導，當用 S100A9 轉基因小鼠進行測試時，12-O-tetradecanoyl phorbol-13-acetate (TPA) 治療增加了表皮癌變過程中未成熟骨髓細胞的積累和乳頭狀瘤的形成（對腫瘤形成很重要）[4]。

Protein kinase C was assayed by measuring the incorporation of 32P into H1 histone from [γ-32P]ATP. The standard reaction mixture (0.25 ml) contained 5 pmol of Tris/HCl at pH 7.5, 1.25 pmol of magnesium nitrate, 50 pg of H1 histone, 2.5 nmol of [γ-32P]ATP (5 to 15xl04 cpm/nmol), and 0.5 pg of protein kinase C. Phospholipid, diolein, phorbol esters, and Ca2+ were added as indicated in each experiment. All reagents were taken up in water which was prepared by a double distillation apparatus followed by passing through a Chelex 100 column to remove as much Ca2+ as possible. After incubation for 3 min at 30oC, the reaction was stopped by the addition of 25% trichloroacetic acid, and acid-precipitable materials were collected on a Toyo-Roshi membrane filter (pore size, 0.45 pm). The catalytic fragment of protein kinase C was assayed similarly except that Ca2+, phospholipid, and diolein were omitted.

Storage	Store at -20°C
M.Wt	616.83
Cas No.	16561-29-8
Formula	C36H56O8
Solubility	insoluble in H2O; ≥112.9 mg/mL in DMSO; ≥80 mg/mL in EtOH
Chemical Name	(1aR,1bS,4aR,7aS,7bS,8R,9R,9aS)-9a-acetoxy-4a,7b-dihydroxy-3-(hydroxymethyl)-1,1,6,8-tetramethyl-5-oxo-1a,1b,4,4a,5,7a,7b,8,9,9a-decahydro-1H-cyclopropa[3,4]benzo[1,2-e]azulen-9-yl tetradecanoate
SDF	Download SDF

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