All Photos(1)
Synonym(s):
NOX Inhibitor VII, Thr101, NADPH Oxidase Inhibitor VII, 6-Fluoro-2- o-tolylbenzo[d]isothiazol-3(2H)-one, 6-Fluoro-2-(2-methylphenyl)-1,2-benzothiazol-3(2H)-one
Empirical Formula (Hill Notation):
C14H10FNOS
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light brown
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable, selenium-to-sulfur substituted Ebselen (Cat. No. 324483) derivative that exhibits similar NOX2 inhibitory activity as Ebselen by blocking p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction. Although less potent than Ebselen in cell-free p22phox PRD-p47phoxbis-SH3 binding (IC50 = 4 vs. 0.3 µM) and NOX2 activity (IC50 = 4 vs. 0.6 µM) assays, Thr101 is more potent and NOX2-selective than Ebselen in cell-based assays (Thr101 IC50 /Ebselen IC50 = 0.3/0.5, 3/0.15, 8/no inhibition, 8/0.7 µM, respectively, against NOX2, NOX1, NOX4, and NOX5) and exhibits no glutathione peroxidase activity.
A cell-permeable, selenium-to-sulfur substituted Ebselen (Cat. No. 324483) derivative that exhibits similar NOX2 inhibitory activity as Ebselen by blocking p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction. Although less potent than Ebselen in cell-free p22phox PRD-p47phoxbis-SH3 binding (IC50 = 4 vs. 0.3 µM) and NOX2 activity (IC50 = 4 vs. 0.6 µM) assays, Thr101 is more potent and NOX2-selective than Ebselen in cell-based assays (Thr101 IC50 /Ebselen IC50 = 0.3/0.5, 3/0.15, 8/no inhibition, 8/0.7 µM, respectively, against NOX2, NOX1, NOX4, and NOX5) and exhibits no glutathione peroxidase activity.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
blocks p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction
blocks p22phox c-terminal PRD (proline-rich domain) and p47phoxbis-SH3 interaction
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Smith, S.M.E., et al. 2012. Chem. Biol.19, 752.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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