MG-101 (ALLN)

製品コードS7386 バッチS738605

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 77 mg/mL (200.76 mM)
Ethanol 39 mg/mL (101.68 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) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
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), and thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. [1] As an inhibitor of Ca(2+)-dependent cysteine proteases, it inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. [2] In HCT116 cells, this compound decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria. [3]
in vivo In mice bearing HCT116 xenografts, this compound (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 Cell 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting stress induction of GRP78 by cardiac glycoside oleandrin dually suppresses cancer and COVID-19 [ Cell Biosci, 2024, 14(1):115] PubMed: 39238058
CUL4B-DDB1-COP1-mediated UTX downregulation promotes colorectal cancer progression [ Exp Hematol Oncol, 2023, 12(1):77] PubMed: 37679762
CUL4B-DDB1-COP1-mediated UTX downregulation promotes colorectal cancer progression [ Exp Hematol Oncol, 2023, 12(1):77] PubMed: 37679762
Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy [ Comput Struct Biotechnol J, 2022, 20:2442-2454] PubMed: 35602976
Assembly and stability of IFT-B complex and its function in BBSome trafficking [ iScience, 2022, 25(12):105493] PubMed: 36411782
Nannocystin ax, an eEF1A inhibitor, induces G1 cell cycle arrest and caspase-independent apoptosis through cyclin D1 downregulation in colon cancer in vivo [ Pharmacol Res, 2021, S1043-6618(21)00454-0] PubMed: 34500061
Tunicamycin Induces Hepatic Stellate Cell Apoptosis Through Calpain-2/Ca2 +-Dependent Endoplasmic Reticulum Stress Pathway [ Front Cell Dev Biol, 2021, 9:684857] PubMed: 34604209
Tunicamycin Induces Hepatic Stellate Cell Apoptosis Through Calpain-2/Ca2 +-Dependent Endoplasmic Reticulum Stress Pathway [ Front Cell Dev Biol, 2021, 9:684857] PubMed: 34604209
SMAD-specific E3 ubiquitin ligase 2 promotes angiogenesis by facilitating PTX3 degradation in MSCs from patients with ankylosing spondylitis [ Stem Cells, 2021, 10.1002/stem.3332] PubMed: 33547700
Suppression of ER-stress induction of GRP78 as an anti-neoplastic mechanism of the cardiac glycoside Lanatoside C in pancreatic cancer: Lanatoside C suppresses GRP78 stress induction [ Neoplasia, 2021, 23(12):1213-1226] PubMed: 34768108

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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