MG-101 (ALLN)

製品コードS7386 バッチS738602

化学情報

	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	5 mg/mL (13.03 mM)


* <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. MG-101 (ALLN) shows very weak inhibitory activities towards cathepsin D (aspartic protease) and subtilisin (serine protease). MG-101 thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. ^[1] MG-101, as an inhibitor of Ca(2+)-dependent cysteine proteases, inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. ^[2] In HCT116 cells, MG-101 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, MG-101 (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 typesare seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of 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

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：

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
Identification of Required Host Factors for SARS-CoV-2 Infection in Human Cells [ Cell, 2020, S0092-8674(20)31394-5]	PubMed: 33147445

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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