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NSC632839
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NSC632839图片
CAS NO:157654-67-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 303.40
Formula C21H21NO
CAS No. 157654-67-6 (HCl)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>5 mg/mL
Water: N/A
Ethanol: N/A
Chemical Name 3,5-Bis[(4-methylphenyl)methylene]-4-piperidone
Synonyms NSC-632839; NSC 632839; NSC632839
SMILES Code O=C1/C(CNC/C1=C\C2=CC=C(C)C=C2)=C/C3=CC=C(C)C=C3
实验参考方法
In Vitro

In vitro activity: NSC632839 is a nonselective isopeptidase inhibitor that inhibits USP2, USP7, and SENP2 with EC50 values of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively. NSC632839 is not only a DUB (deubiquitylases) inhibitor, but also a deSUMOylase inhibitor. Conjugation or deconjugation of ubiquitin (Ub) or ubiquitin-like proteins (UBLs) to or from cellular proteins is a multifaceted and universal means of regulating cellular physiology, controlling the lifetime, localization, and activity of many critical proteins. Deconjugation of Ub or UBL from proteins is performed by a class of proteases called isopeptidases. The inhibitory activity of the nonselective isopeptidase inhibitor NSC 632839 against deubiquitylases and deSUMOylases was profiled.


Kinase Assay: 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.


Cell Assay: 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.

In Vivo
Animal model
Formulation & Dosage
References Biochem Biophys Res Commun. 2018 Mar 4;497(2):726-733; Protein Sci. 2008 Jun;17(6):1035-43.