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NSC632839

Catalog No. T3951   CAS 157654-67-6
Synonyms: F6, Ubiquitin Isopeptidase Inhibitor II

NSC-632839 (Ubiquitin Isopeptidase Inhibitor II) is a nonselective isopeptidase inhibitor, which inhibits USP2 (EC50: 45±4 μM), USP7 (EC50: 37±1 μM), and SENP2 (EC50: 9.8±1.8 μM).

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NSC632839 Chemical Structure
NSC632839, CAS 157654-67-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 72.00
25 mg In stock $ 153.00
50 mg In stock $ 273.00
100 mg In stock $ 415.00
500 mg In stock $ 942.00
1 mL * 10 mM (in DMSO) In stock $ 47.00
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Purity: 99.87%
Purity: 99.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NSC-632839 (Ubiquitin Isopeptidase Inhibitor II) is a nonselective isopeptidase inhibitor, which inhibits USP2 (EC50: 45±4 μM), USP7 (EC50: 37±1 μM), and SENP2 (EC50: 9.8±1.8 μM).
Targets&IC50 USP7:37±1 μM(EC50), USP2:45±4 μM(EC50), SENP2:9.8±1.8 μM(EC50)
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. NSC 632839 (1.2-150 μM) does not inhibit the PLA2, indicating that the inhibition for isopeptidases is selective.
Kinase Assay 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].
Synonyms F6, Ubiquitin Isopeptidase Inhibitor II
Molecular Weight 339.86
Formula C21H22ClNO
CAS No. 157654-67-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.25 mg/mL (18.39 mM)

TargetMolReferences and Literature

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

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Target-Focused Phenotypic Screening Library HIF-1 Signaling Pathway Compound Library Anti-Aging Compound Library Bioactive Compound Library Anti-Cancer Compound Library DNA Damage & Repair Compound Library Cell Cycle Compound Library Ubiquitination Compound Library Bioactive Compounds Library Max

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Keywords

NSC632839 157654-67-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB F 6 NSC-632839 inhibit F6 NSC 632839 Inhibitor DUBs Ubiquitin Isopeptidase Inhibitor II Deubiquitinase F-6 inhibitor

 

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