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NSC 632839 hydrochloride Isopeptidases inhibitor

Catalog No.A4004
Size Price Stock Qty
10mg
$70.00
In stock
50mg
$230.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

NSC 632839 hydrochloride

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Chemical Properties

Cas No. 157654-67-6 SDF Download SDF
Synonyms N/A
Chemical Name (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
Formula C21H21NO.HCl M.Wt 339.86
Solubility ≥17 mg/mL in DMSO with gentle warming, <2.48 mg/mL in EtOH, <2.36 mg/mL in H2O Storage Store at 4°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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.