NSC632839 - Deubiquitinase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENSC632839Cat. No.: HY-100708CAS No.: 157654-67-6分式: CHClNO分量: 339.86作靶點(diǎn): Deubiquitinase作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6.2 mg/mL (18.24 mM; Need wa

2、rming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.9424 mL 14.7119 mL 29.4239 mL5 mM 0.5885 mL 2.9424 mL 5.8848 mL10 mM 0.2942 mL 1.4712 mL 2.9424 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NSC632839種選擇性肽酶抑制劑，抑制 USP2，USP7 和 SENP2，EC50 分別為 454 M，371 M和 9.81.8 M。IC50

3、& Target EC50: 454 M (USP2), 371 M (USP7), 9.81.8 M (SENP2) 1體外研究NSC 632839 inhibits ubiquitin isopeptidases as illustrated by its ability to inhibit z-LRGG-AMC cleavage bycrude lysates in the mid-micromolar range. To further characterize NSC 632839 against purified enzymes, its1/2 Master of Small M

4、olecules 您邊的抑制劑師www.MedChemEinhibitory potential is determined against purified USP2, USP7, and SENP2 and demonstrated that NSC632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor. Specifically, NSC 632839 inhibitsUSP2, USP7, and SENP2 with EC50 values of 454 M, 371 M, and 9.81.8 M,

5、respectively.Importantly, NSC 632839 does not inhibit the reporter enzyme PLA2 over the concentration range tested(1.2-150 M), indicating that the reported inhibition is selective for isopeptidases. Moreover, the isopeptidaseinhibitory activity of NSC 632839 is confirmed by the observation that it d

6、oes not inhibit free PLA2 over theconcentration range tested 1.PROTOCOLKinase Assay 1 In a 96-well-plate, 40 nM USP2, 40 nM USP7, or 20 nM SENP2 is preincubated with a concentration range ofNSC 632839 (NCI/NIH developmental therapeutics program) or control for 30 min before supplementationwith an eq

7、ual volume of 60 nM Ub-PLA2/40 M NBD C6-HPC (USP2 or 7) or 20 nM SUMO3-PLA2/40 MNBD C6-HPC (SENP2). Relative activity of the enzymes is determined by measuring the RFU values atsingle time points within the initial linear range (USP, 50 min; USP7, 50 min; and SENP2, 30 min). The RFUvalues within the

8、 initial linear range are normalized such that isopeptidase+vehicle=0% inhibition andisopeptidase+NEM=100% inhibition. The EC50 values are determined as above. The inhibitory activity of thetest compound against the reporter enzyme PLA2 is performed as described above except there is nopreincubation

9、 step and the data are normalized such that free PLA2+vehicle=0% inhibition and freePLA2+EDTA=100% inhibition. PLA2 activity is determined 8 min after the addition of the reagents 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Biochem Bio

10、phys Res Commun. 2018 Mar 4;497(2):726-733.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nicholson B, et al. Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities. Protein Sci. 2008 Jun;17(6):1035-43.McePdfHeightCaution: Product has not been fully valida