NSC632839

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

泛素蛋白酶体系统的小分子抑制剂，通过抑制泛素肽酶来实现。

A small molecule inhibitor of ubiquitin-proteasome system by inhibiting the ubiquitin isopeptidases; induce a unique apoptotic pathway, which includes a Bcl-2-dependent but apoptosome-independent mitochondrial pathway with up-regulation of the BH3-only protein Noxa, stabilization of the IAP antagonist Smac, but also the involvement of the death receptor pathway.

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.

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NSC-632839 | NSC 632839 | Ubiquitin Isopeptidase-IN-F6

Proteasome/Ubiquitin

DUB

SENP2|USP2|USP7

Cancer

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157654-67-6

339.8585

C21H22ClNO

>98% (HPLC)

DMSO: 6.2 mg/mL (Need warming)

CC1=CC=C(C=C1)C=C2CNCC(=CC3=CC=C(C=C3)C)C2=O.Cl

4-Piperidinone, 3,5-bis[(4-methylphenyl)methylene]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years