NSC 632839,157654-67-6

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YZ剂描述：

产品名称：NSC 632839

产品别名：(3E,5E)-3,5-bis[(4-methylphenyl)methylidene]piperidin-4-one,hydrochloride

英文别名：NSC632839 hydrochloride

靶点：DUB

CAS：157654-67-6

纯度：>98%

外观：黄色固体

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

NSC 632839不仅是一种DUBYZ剂，也是一种deSUMOylaseYZ剂，作用于USP2， USP7，和SENP2， IC50分别为45 μM， 37 μM和9.8 μM。NSC 632839 YZ纯化的USP2-和USP7调节的Ub-PLA2裂解。在实验浓度范围内（1.2-150 μM）不YZ受体酶PLA2，说明NSC 632839选择性YZ异肽酶。 NSC 632839作用于E1A和E1A/C9DN细胞，在没有功能性caspase-9存在时，能够维持caspase-3/caspase-7活性。

溶解性：DMSO ：6.2 mg/mL

体外研究：

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.

体内研究：

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