1. Apoptosis Stem Cell/Wnt MAPK/ERK Pathway
  2. Apoptosis ERK
  3. FR900359

FR900359 是一种酯肽,是哺乳动物 q/11/14 的选择性抑制剂,能抑制 ERK 通路,能抑制黑色素瘤细胞增殖,降低血压。在 Ovalbumins (HY-W250978) 诱导的过敏性小鼠哮喘模型中,FR900359 也能防止气道过度反应。FR900359 可用于癌症和心血管疾病研究。

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FR900359 Chemical Structure

FR900359 Chemical Structure

CAS No. : 107530-18-7

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250 μg(997.84 μM * 250 μL in Acetonitrile) ¥2610
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查看 ERK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FR900359 is a depsipeptide selective inhibitor of q/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4].

体外研究
(In Vitro)

FR900359 (1.0 μM,1 小时) 在 HEK293 细胞中抑制 Gαq、Gα11 和 Gα/14,但不抑制 Gα<16 或任何其他哺乳动物 Gα 亚型[1]
FR900359 (0-10 μM, 24 小时) 以浓度依赖的方式有效地减少 B16 细胞的生长,抑制增殖及迁移[1]
FR900359 (10 nM, 72 小时) 诱导黑色素瘤细胞 G1 细胞周期停滞,使其分化[1]
FR900359 (1.0 μM, 5 分钟) 阻断 Gq 依赖性 ERK1/2 激活[1]
FR900359 (1 μM, 24 小时) 与未处理组相比,显著诱导更多的 92.1 细胞发生凋亡[3]
FR900359 (30 nM,60 分钟) 诱导小鼠、猪和人体外气道发生剂量依赖性松弛[4]

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

Cell Proliferation Assay[1]

Cell Line: B16 cells
Concentration: 0-10 μM
Incubation Time: 24 hours
Result: Effectively reduced growth of B16 cells in a concentration-dependent manner and suppressed cell proliferation and migration.

Cell Differentiation Assay[1]

Cell Line: B16 cells
Concentration: 10 nM
Incubation Time: 72 hours
Result: Induced G1 cell cycle arrest in melanoma cells with Gq tone.
Treated cells appeared flattened, rather dark, and packed with melanin vesicles, attributes consistent with the adoption of a more differentiated state.
Made melanocyte differentiation marker gp100 was upregulated considerably on FR treatment.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1.0 μM
Incubation Time: 5 min
Result: FR interdicts Gq-dependent ERK1/2 activation

Apoptosis Analysis[3]

Cell Line: 92.1 cells
Concentration: 1.0 μM
Incubation Time: 24 hours
Result: Significantly induced more 92.1 cells undergoing apoptosis compared to untreated cells
体内研究
(In Vivo)

FR900359 (0.2 或1 mg/ml, 每只鼠 12 μL, 静脉注射) 显著降低小鼠尾静脉血管张力[1]
FR900359 (0.1 mg/ml,2.5 mg/小鼠,气管内给药) 消除了 Ovalbumin (HY-W250978) 诱导的小鼠致敏后的气道高反应性[4]

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

Animal Model: Isometric force measurements in mouse tail artery [1]
Dosage: 1.0 μM
Administration: Washed
Result: Strongly reduced vascular tone
Animal Model: Ovalbumins–induced sensitization model of asthma. [4]
Dosage: 0.1 mg/ml, 2.5 mg per mouse
Administration: Intratracheally
Result: Abolished airway hyperreactivity after ovalbumin-induced sensitization in mice
分子量

1002.16

Formula

C49H75N7O15

CAS 号
性状

液体

颜色

Colorless to light yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years

纯度 & 产品资料

纯度: ≥99.0%

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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产品名称:
FR900359
目录号:
HY-117037
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