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NSC 632839 hydrochloride Sale

(Synonyms: F6, Ubiquitin Isopeptidase Inhibitor II) 目录号 : GC12475

A deubiquitylase and deSUMOylase inhibitor

NSC 632839 hydrochloride Chemical Structure

Cas No.:157654-67-6

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10mg
¥525.00
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50mg
¥1,607.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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].

References:

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

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:
[1] Nicholson B, Leach CA, Goldenberg SJ, Francis DM, Kodrasov MP, Tian X, Shanks J, Sterner DE, Bernal A, Mattern MR, Wilkinson KD, Butt TR. Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities. Protein Sci. 2008 Jun;17(6):1035-43.
[2] Gupta-Saraf P, Miller CL. HIF-1α downregulation and apoptosis in hypoxic prostate tumor cells infected with oncolytic mammalian orthoreovirus. Oncotarget. 2014 Jan 30;5(2):561-74.
[3] Eldridge AG, O'Brien T. Therapeutic strategies within the ubiquitin proteasome system. Cell Death Differ. 2010 Jan;17(1):4-13.

Chemical Properties

Cas No. 157654-67-6 SDF
别名 F6, Ubiquitin Isopeptidase Inhibitor II
化学名 (3E,5E)-3,5-bis[(4-methylphenyl)methylidene]piperidin-4-one;hydrochloride
Canonical SMILES CC1=CC=C(C=C1)C=C2CNCC(=CC3=CC=C(C=C3)C)C2=O.Cl
分子式 C21H21NO.HCl 分子量 339.86
溶解度 ≥ 17 mg/mL in DMSO with gentle warming 储存条件 Store at 4°C
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储备液的保存方式和期限:-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。
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1 mM 2.9424 mL 14.7119 mL 29.4239 mL
5 mM 0.5885 mL 2.9424 mL 5.8848 mL
10 mM 0.2942 mL 1.4712 mL 2.9424 mL
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