| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
Kinase experiment: | 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]. |
| 产品描述 | NSC 632839 is a nonselective inhibitor of isopeptidases with IC50 values of 45 μM, 37μM, and 9.8μM, respectively for USP2, USP7, and SENP2 [1]. NSC 632839 is reported to have activity against the purified isopeptidases. It inhibits not only DUB (USP2, USP7) but also deSUMOylase (SENP2). It is also shown to inhibit cleavage of an Ub mimetic (z-LRGG-AMC) by transformed fibroblast lysates. However, NSC 632839 has no inhibition to the reporter enzyme PLA2, suggesting the inhibition is selective for isopeptidases [1]. NSC 632839 prevents removal of ubiquitin chains from polyubiquitinated proteins, inhibiting ubiquitin-dependent, proteasome-mediated degradation. It activates apoptosis in an apoptosome-independent manner [2, 3]. References: |
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