NSC632839


Catalog No. Size PriceQuantity
M13476-2 2mg solid $95
M13476-10 10mg solid $285

Description

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.

Product information

CAS Number: 157654-67-6

Molecular Weight: 339.86

Formula: C21H22ClNO

Chemical Name: (3E,5E)-3,5-bis[(4-methylphenyl)methylidene]piperidin-4-one; chlorohydrogen

Smiles: Cl.CC1C=CC(/C=C2\CNC/C(=C\C3C=CC(C)=CC=3)/C\2=O)=CC=1

InChiKey: ZOKZLTXPTLIWOJ-BYCVLTJGSA-N

InChi: InChI=1S/C21H21NO.ClH/c1-15-3-7-17(8-4-15)11-19-13-22-14-20(21(19)23)12-18-9-5-16(2)6-10-18;/h3-12,22H,13-14H2,1-2H3;1H/b19-11+,20-12+;

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

References:

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

Products are for research use only. Not for human use.

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