NSC 632839

製品コードS4922 バッチS492201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H21NO.HCl
分子量 339.86 CAS No. 157654-67-6
Solubility (25°C)* 体外  
 
 
* <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.

生物活性

製品説明 NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, it inhibits USP2, USP7, and SENP2 with EC50 of 45 μM, 37 μM, and 9.8 μM, respectively.
in vitro NSC 632839 inhibits purified USP2- and USP7-mediated cleavage of Ub-PLA2. NSC 632839 does not inhibit the reporter enzyme PLA2 over the concentration range tested (1.2–150 μM), indicating that the reported inhibition is selective for isopeptidases. [1] NSC 632839 is capable of sustaining caspase-3/caspase-7 activity in the absence of a functional caspase-9 in E1A and E1A/C9DN cells. NSC 632839 induces apoptosis with IC50 of 15.65 μM and 16.23 μM in E1A and E1A/C9DN cells, respectively. NSC-632839 (10 μM) provokes the accumulation of polyubiquitins in E1A cells expressing HA-tagged ubiquitin. NSC-632839 (10 μM) dramatically increases the levels of Noxa and Mcl-1 in E1A cells during a time course analysis. NSC-632839 (10 μM) provokes mitochondrial fragmentation in a higher percentage of cells with an intact outer mitochondrial membrane compared with etoposide. [2]
特徴 Less potent than NSC 144303 in inducing apoptosis of E1A and E1A/C9DN cells.
密度 g/mL

プロトコル(参考用のみ)

キナーゼアッセイ Characterization of NSC 632839
In a 96-well-plate, 40 nM USP2, 40 nM USP7, or 20 nM SENP2 is preincubated with a concentration range of NSC 632839 or control for 30 min before supplementation with an equal volume of 60 nM Ub-PLA2/40 μM NBD C6-HPC (USP2 or 7) or 20 nM SUMO3-PLA2/40 μM NBD C6-HPC (SENP2). Relative activity of the enzymes is determined by measuring the RFU values at single time points within the initial linear range (USP, 50 min; USP7, 50 min; and SENP2, 30 min). The RFU values within the initial linear range are normalized such that isopeptidase + vehicle = 0% inhibition and isopeptidase + NEM = 100% inhibition.

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。