NSC632839
Based on 3 publication(s) in Google Scholar
NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.12%
- CAS 番号: 157654-67-6
- 分子式: C21H22ClNO
- 分子量:339.86
-
保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Ubiquitination Compound Library
HY-L050
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Cysteine Targeted Covalent Library
HY-L153
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 NSC632839
More
Customer Validation & Images
-
IF
-
WB
生物活性
EC50: 45±4 μM (USP2), 37±1 μM (USP7), 9.8±1.8 μM (SENP2)[1]
NSC 632839 inhibits ubiquitin isopeptidases as illustrated by its ability to inhibit z-LRGG-AMC cleavage by crude lysates in the mid-micromolar range. To further characterize NSC 632839 against purified enzymes, its inhibitory potential is determined against purified USP2, USP7, and SENP2 and demonstrated that NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor. Specifically, NSC 632839 inhibits USP2, USP7, and SENP2 with EC50 values of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively. Importantly, 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. Moreover, the isopeptidase inhibitory activity of NSC 632839 is confirmed by the observation that it does not inhibit free PLA2 over the concentration range tested[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 157654-67-6
-
性状 Solid
-
分子量 339.86
-
分子式 C21H22ClNO
-
Color Light yellow to yellow
-
SMILES
O=C1/C(CNC/C1=C\C2=CC=C(C)C=C2)=C/C3=CC=C(C)C=C3.[H]Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Cell Chem Biol
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2. [Abstract]2021 Jun 17;28(6):855-865.e9. PMID: 33979649 -
J Med Chem
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]2022 Oct 27;65(20):13645-13659. PMID: 36221183 -
Biochem Biophys Res Commun
Ubiquitin C-Terminal Hydrolase L1 regulates autophagy by inhibiting autophagosome formation through its deubiquitinating enzyme activity. [Abstract]2018 Mar 4;497(2):726-733. PMID: 29462615
NSC632839 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733. [Abstract]
Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. mRFP-GFP-LC3 stable cell line is treated with 5 μM LDN or 10 μM NSC in the condition of DMSO or Torin1 respectively for 6 h. The number of LC3 puncta remarkably is raised both in LDN and NSC treatment cells compared to the control.
NSC632839 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733. [Abstract]
Drug screen of UCHL1 and the function of inhibitors in autophagy. Both LDN and NSC could inhibit UCHL1 hydrolase activity. Each cell lysate is analyzed by immunoblotting with anti p62 and LC3 antibodies.
溶剤 & 溶解度
DMSO : 4 mg/mL (11.77 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
In a 96-well-plate, 40 nM USP2, 40 nM USP7, or 20 nM SENP2 is preincubated with a concentration range of NSC 632839 (NCI/NIH developmental therapeutics program) 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. The EC50 values are determined as above. The inhibitory activity of the test compound against the reporter enzyme PLA2 is performed as described above except there is no preincubation step and the data are normalized such that free PLA2+vehicle=0% inhibition and free PLA2+EDTA=100% inhibition. PLA2 activity is determined 8 min after the addition of the reagents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (274 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9424 mL | 14.7119 mL | 29.4239 mL | 73.5597 mL |
| 5 mM | 0.5885 mL | 2.9424 mL | 5.8848 mL | 14.7119 mL | |
| 10 mM | 0.2942 mL | 1.4712 mL | 2.9424 mL | 7.3560 mL |
NSC632839 関連分類
HY-100708 関連分類
Powered by Bioz