Marizomib (Salinosporamide A)

製品コードS7504 バッチS750401

印刷

化学情報

Chemical Structure Synonyms ML858, MRZ, NPI-0052 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C15H20ClNO4
分子量 313.78 CAS No. 437742-34-2
Solubility (25°C)* 体外 DMSO 63 mg/mL (200.77 mM)
 
 
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Marizomib (Salinosporamide A) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM.
in vitro

Marizomib inhibits the proteasome activity, proliferation, and invasion of glioma cells. Meanwhile, free radical production and apoptosis induced by marizomib can be blocked by antioxidant N-acetyl cysteine.[1]
in vivo

In animal studies, marizomib distributes into the brain at 30% of blood levels in rats and significantly inhibits (>30%) baseline chymotrypsin-like proteasome activity in brain tissue of monkeys. Encouragingly, the immunocompromised mice, intracranially implanted with glioma xenografts, survives significantly longer than the control animals when treated with marizomib.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 The human glioma cell lines U-251 MG and D-54 MG
濃度 60 nM
反応時間 2 h, 24 h
実験の流れ

Proteasome activity is measured in neural stem cells and glioblastoma-derived glioma stem cells at baseline and 2 hours after treatment with marizomib (60 nM). Invasion capability of U-251 MG and D-54 MG cells treated or untreated with 60 nM marizomib for 24 hours is analyzed using Matrigel invasion chambers.
動物実験 動物モデル male Sprague-Dawley rats, 6–8 week old mice
投薬量 0.1 mg/kg, 200 µg/kg
投与方法 IV

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 mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843] PubMed: 37014128
Targeting mitochondrial energetics reverses panobinostat- and marizomib-induced resistance in pediatric and adult high-grade gliomas [ Mol Oncol, 2023, 17(9):1821-1843] PubMed: 37014128
Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 11(5):e0190423] PubMed: 37750732
Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 10.1128/spectrum.01904-23] PubMed: 37750732
Collateral deletion of the mitochondrial AAA+ ATPase ATAD1 sensitizes cancer cells to proteasome dysfunction [ Elife, 2022, 11e82860] PubMed: 36409067
Targeting NAD+ Biosynthesis Overcomes Panobinostat and Bortezomib-Induced Malignant Glioma Resistance [ Mol Cancer Res, 2020, 18(7):1004-1017] PubMed: 32238439

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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