MG-101 (ALLN)

製品コードS7386 バッチS738601

印刷

化学情報

Chemical Structure Synonyms Calpain inhibitor-1, Ac-LLnL-CHO Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H37N3O4
分子量 383.53 CAS No. 110044-82-1
Solubility (25°C)* 体外 DMSO 76 mg/mL (198.15 mM)
Ethanol 76 mg/mL (198.15 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) は、カルパインやリソソームカテプシンを含むシステインプロテアーゼの細胞透過性で強力な阻害剤です。
in vitro MG-101 (ALLN) effectively inhibits cysteine proteinases with ID50 of 7 nM and 13 nM for cathepsins L and B, respectively. This compound shows very weak inhibitory activities towards cathepsin D (aspartic protease) and subtilisin (serine protease). It thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. As an inhibitor of Ca(2+)-dependent cysteine proteases, this chemical inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. In HCT116 cells, it decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria.
in vivo In mice bearing HCT116 xenografts, MG-101 (ALLN) (10 mg/kg i.p.) inhibits colon tumor formation. [3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116, HCT116/p53−/−, and HCT116/Bax−/− cells
濃度 ~26 μM
反応時間 24 hours
実験の流れ Cells viability is assayed using Cell Counting Kit-8 following manufacturer’s protocol. All HCT116 cell types are seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of MG-101 (ALLN) for 24 h. Medium is then replaced by 100 μl fresh McCoy’s 5A complete medium with 10% CCK-8 reagent and incubated for 1 h. Absorbance is measured at 450 nm using a microplate reader. Results are shown as death percentages.
動物実験 動物モデル Female athymic nude mice bearing HCT116 xenografts
投薬量 10 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/2403861/
  • https://pubmed.ncbi.nlm.nih.gov/1906466/
  • https://pubmed.ncbi.nlm.nih.gov/23831472/

カスタマーフィードバック

Data from [Data independently produced by , , Graefes Arch Clin Exp Ophthalmol, 2018, 257(1):83-94]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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