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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

339.86

C₂₁H₂₂ClNO

157654-67-6

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

DMSO : 6.2 mg/mL (18.24 mM; Need warming)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

• [1]. Nicholson B, et al. Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities. Protein Sci. 2008 Jun;17(6):1035-43.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Nicholson B, et al. Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities. Protein Sci. 2008 Jun;17(6):1035-43.