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  3. 12-Deoxyphorbol-13-isobutyrate-20-acetate

12-Deoxyphorbol-13-isobutyrate-20-acetate 是一种 12-脱氧佛波醇二萜酯。12-Deoxyphorbol-13-isobutyrate-20-acetate 是一种蛋白激酶 C (PKC) 激动剂,可激活 PKC肌钙蛋白 I肌钙蛋白 T 进行磷酸化修饰。12-Deoxyphorbol-13-isobutyrate-20-acetate 可诱导小鼠皮肤刺激和坏死,但不具有促癌活性。12-Deoxyphorbol-13-isobutyrate-20-acetate 可抑制炭黑曲霉的生长。12-Deoxyphorbol-13-isobutyrate-20-acetate 可用于心力衰竭、心肌病和真菌感染相关研究。

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12-Deoxyphorbol-13-isobutyrate-20-acetate

12-Deoxyphorbol-13-isobutyrate-20-acetate Chemical Structure

CAS No. : 25090-71-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

12-Deoxyphorbol-13-isobutyrate-20-acetate is a 12-deoxy-phorbol diterpene ester. 12-Deoxyphorbol-13-isobutyrate-20-acetate is a protein kinase C (PKC) agonist that activates protein kinase C to phosphorylate troponin I and troponin T. 12-Deoxyphorbol-13-isobutyrate-20-acetate induces skin irritation and necrosis in mice without cocarcinogenic activity. 12-Deoxyphorbol-13-isobutyrate-20-acetate inhibits Aspergillus carbonarius growth. 12-Deoxyphorbol-13-isobutyrate-20-acetate supports research on heart failure, cardiomyopathies and fungal infection[1][2][3].

IC50 & Target[1]

PKC

 

体外研究
(In Vitro)

12-Deoxyphorbol-13-isobutyrate-20-acetate (1 μM) 可通过非钙依赖机制降低完整人心小梁的收缩力,且咖啡因可部分逆转其负性肌力作用及肌丝钙敏感性的降低[1]
12-Deoxyphorbol-13-isobutyrate-20-acetate (1 μM) 可降低去膜人心室肌小梁的肌丝钙敏感性 (将 [Ca2+]50% 偏移至 2.09 μM 并降低最大收缩力),同时在 [Ca2+]50% 持续升高的情况下,降低完整的对照组和肌病组人心室肌小梁的收缩力并改变希尔系数[1]
12-Deoxyphorbol-13-isobutyrate-20-acetate (10-100 μM; 3 days) 可使 Aspergillus carbonarius 的生长量降低 25%[3]
12-Deoxyphorbol-13-isobutyrate-20-acetate (0.001-100 μM; 72 h) 可相似程度地降低 MCF7 乳腺癌细胞和 MCF10A 正常乳腺细胞的活力,对癌细胞无选择性细胞毒性[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[3]

Cell Line: MCF7 breast cancer cells, MCF10A normal breast cells
Concentration: 0.001 μM, 1 μM, 10 μM, 100 μM
Incubation Time: 72 h
Result: Reduced viability of MCF7 breast cancer cells and MCF10A normal breast cells to a similar extent, with no significant difference in cytotoxicity between the two cell lines at any tested concentration.
体内研究
(In Vivo)

12-Deoxyphorbol-13-isobutyrate-20-acetate (每耳 0.024 nmoles;局部给药;单剂量) 在小鼠耳局部刺激模型中诱导发红的 ID50 为 0.024 nmoles per ear[2]
12-Deoxyphorbol-13-isobutyrate-20-acetate (每剂 0.2 μmoles;局部给药;每周 2 次;持续 24 周) 在经 7,12-二甲基苯并[a]蒽启动的 NMRI 小鼠中未表现出可检测到的共致癌促肿瘤活性,24 周内肿瘤发生率为 0%、肿瘤产率为 0,同时死亡率为 28%[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NMRI (female)[2]
Dosage: 0.2 μmoles per dose
Administration: topical; twice weekly; 24 weeks
Result: Resulted in 0% of mice developing tumors at 12 weeks and 24 weeks.
Achieved a tumor yield of 0 tumors per survivor at 12 weeks and 24 weeks.
Caused 28% mortality after 24 weeks.
Induced pronounced skin necrosis in the treated area after 2-3 applications.
分子量

460.56

Formula

C26H36O7

CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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