1. 诱导疾病模型产品 Metabolic Enzyme/Protease
  2. 肿瘤模型 神经系统疾病模型 Phosphatase
  3. 皮肤肿瘤模型 阿尔兹海默症模型
  4. Okadaic acid ammonium salt

Okadaic acid ammonium salt  (Synonyms: 冈田酸铵盐)

目录号: HY-115760
产品使用指南

Okadaic acid ammonium salt 是一种海洋毒素,是蛋白质磷酸酶 (PP) 的抑制剂,包括 PP1 (IC50=15-50 nM)、PP2A (IC50=0.1-0.3 nM)、PP3 (IC50=3.7-4 nM)、PP4 (IC50=0.1 nM) 和 PP5 (IC50=3.5 nM),其中对 PP2A 的亲和力最显著,但不抑制 PP2C。Okadaic acid ammonium salt 通过抑制 PP 增加了多种蛋白的磷酸化,并具有肿瘤启动子的作用。Okadaic acid ammonium salt 诱导 tau 蛋白磷酸化。

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Okadaic acid ammonium salt Chemical Structure

Okadaic acid ammonium salt Chemical Structure

CAS No. : 175522-42-6

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Other Forms of Okadaic acid ammonium salt:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Okadaic acid ammonium salt, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid ammonium salt has a significantly higher affinity for PP2A (IC50=0.1-0.3 nM), and inhibits PP1 (IC50=15-50 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), but does not inhibit PP2C. Okadaic acid ammonium salt increases of phosphorylation of a number of proteins by inhibiting PP, and acts as a tumor promoter. Okadaic acid ammonium salt induces tau phosphorylation[1][2].

IC50 & Target[1]

PP1

15-50 nM (IC50)

PP2A

0.1-0.3 nM (IC50)

PP3

3.7-4 nM (IC50)

PP4

0.1 nM (IC50)

PP5

3.5 nM (IC50)

PP2B

~4000 nM (IC50)

PP7

>1000 nM (IC50)

体外研究
(In Vitro)

Okadaic acid ammonium salt (0-100 nM; 24 h or 48 h) inhibits the proliferation of AGS, MNK-45, Caco 2 cells[3].
Okadaic acid (10 nM, 8 hours) ammonium salt increases Drp1 phosphorylation and mitochondrial fission in rat cortical neurons[4].

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

Cell Proliferation Assay[3]

Cell Line: AGS, MNK-45 and Caco 2 cell lines
Concentration: 0-100 nM
Incubation Time: 24 h or 48 h
Result: Inhibited the proliferation of AGS, MNK-45, Caco 2 cells.
体内研究
(In Vivo)

kadaic acid 可用于动物建模,构建阿尔兹海默症和皮肤肿瘤模型[6][7][8]

1. 诱导神经毒性[6][7]
致病原理
Tau protein hyperphosphorylation is a major pathological hallmark of Alzheimer’s disease (AD). Okadaic acid can induce a decrease in protein phosphatase (PP-2A) activity, leading to tau protein hyperphosphorylation.
具体造模方法:
大鼠:Wistar • 雄性 • 2 个月大
给药方式:200 ng • icv • 单剂量
Note
(1) 将 200ng Okadaic acid 溶解于人工脑脊液(aCSF) 中,人工脑脊液含:147 mmol/L NaCl、2.9 mmol/L KCl、1.6 mmol/L MgCl2、1.7 mmol/L CaCl2、2.2 mmol/L葡萄糖,每只大鼠 aCSF 注射量为10μL。
(2) 脑室内注射Okadaic acid 后,腹腔注射庆大霉素(5mg/kg) 预防脓毒症。
(3) 与缺氧联合治疗可增强 Okadaic acid 的神经毒性作用。缺氧处理方法:脑室内注射 Okadaic acid 后,将大鼠置于缺氧舱中,氧气含量为 10%,每天 22 小时,连续 3 天。
造模成功指标
分子变化:胱天蛋白酶原 3 水平降低,乙酰胆碱酯酶活性和表达降低,胱天蛋白酶 3、β-淀粉样蛋白 (Aβ42) 和磷酸化 tau 蛋白水平升高,ROS 和丙二醛 (MDA) 积累。
表型观察:大鼠脑神经元损伤和死亡,伴随细胞肿胀和核染色质凝聚。
相关产品: /
拮抗产品: /

2. 诱导皮肤肿瘤[8]
致病原理
Okadaic acid 是一种皮肤刺激剂和有毒的聚醚化合物,发挥出非 TPA 型肿瘤促进剂的作用。Okadaic acid 会刺激小鼠耳朵和小鼠皮肤中的鸟氨酸脱羧酶,但不诱导人早幼粒细胞白血病细胞(HL-60细胞)的黏附,不会抑制 [3H]TPA 与小鼠颗粒组分的特异性结合,也不激活蛋白激酶 C[8]
具体造模方法:
小鼠:CD-1 • 雌性 • 8 周龄
给药方式:10 μg • 局部应用 • 每周两次,持续 30 周
Note
(1) 10 μg Okadaic acid 溶解于丙酮,涂抹体积为每只大鼠 0.1 mL。
(2) 对皮肤肿瘤的诱导可分为两个阶段,局部涂抹 Okadaic acid 为第 2 阶段。第 1 阶段处理方式为局部涂抹溶解于丙酮的 DMBA (DMBA含量为 100μg,丙酮体积为 0.1 mL),一周后进行第 2 阶段处理。单独使用 Okadaic acid 与联合使用 Okadaic acid 和 DMBA 均对皮肤肿瘤具有诱导作用,联合使用的诱导效果更佳。
造模成功指标
表型观测:皮肤表面乳头状瘤 (papillomas) 和肉瘤 (sarcoma) 发生率上升。
相关产品DMBA (HY-W011845); Teleocidin
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MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female wild-type C57BL/6 mice (6 to 8 months)[5]
Dosage: 100 μM
Administration: Injected unilaterally to the lateral amygdala
Result: Induced Tau phosphorylation and protein aggregation in anatomically distinct brain regions 24 h post-injection.
分子量

822.03

Formula

C44H71NO13

CAS 号
中文名称

冈田酸铵盐

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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  • 稀释计算器

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Help & FAQs
  • 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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Okadaic acid ammonium salt
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