1. Epigenetics TGF-beta/Smad
  2. PKC
  3. Calphostin A

Calphostin A 是一种光敏性的蛋白激酶 C (protein kinase C) 抑制剂,其 IC50 为 250 nM。Calphostin A 仅在光照条件下发挥蛋白激酶 C 抑制活性,且该活性不受抗氧化剂影响。Calphostin A 可作为膜毒物、自由基生成剂和单线态氧生成剂,在光照时会产生单线态氧和自由基,进而破坏钙稳态、升高静息细胞质钙水平、降低膜输入电阻并增加膜泄漏电流。

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Calphostin A

Calphostin A Chemical Structure

CAS No. : 120461-92-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Calphostin A is a photosensitive protein kinase C inhibitor with an IC50 of 250 nM. Calphostin A exerts protein kinase C inhibitory activity only under light conditions, and this activity is not affected by antioxidants. Calphostin A acts as a membrane toxicant, free radical generator and singlet oxygen generator; under light exposure, it produces singlet oxygen and free radicals, which in turn disrupt calcium homeostasis, elevate resting cytoplasmic calcium levels, reduce membrane input resistance and increase membrane leakage current[1].

体外研究
(In Vitro)

Calphostin A (30-40 nM; 30 min 光照暴露) 可阻断 PMA (HY-18739) 诱导的分化小鼠 N1E-115 神经母细胞瘤细胞中
Carbamoylcholine chloride (HY-B1208) 诱发的钙释放减少,提示其具有光依赖性 PKC 抑制活性[1]
Calphostin A (1 μM; 4-10 min 光照暴露) 会破坏分化的小鼠 N1E-115 神经母细胞瘤细胞中的钙稳态,以光依赖的方式提高静息细胞质钙水平并降低激动剂诱发的钙释放[1]
Calphostin A (1 μM; 场地照明) 可通过一种依赖自由基的机制增加分化的小鼠 N1E-115 神经母细胞瘤细胞的膜漏电流,因为预先用 α-tocopherol (HY-N0683) 处理可阻断该效应[1]

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

分子量

758.77

Formula

C44H38O12

CAS 号
结构分类
初始来源

Cladosporium cladosporioides

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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  • 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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