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Description
Overview
A cell-permeable, trifluoromethyl substituted aromatic hydroxamate compound that acts as a highly potent, selective, mixed type, reversible inhibitor of the chlorination activity of myeloperoxidase (MPO; IC50 = 5 nM). Tightly binds within the active site cavity above the heme and blocks the substrate channel. Displays over 300-fold greater selectivity for MPO when tested against a panel of redox enzymes, including lactoperoxidase (IC50 = 6.3 µM) and thyroid peroxidase (IC50 = 1.59 µM). Blocks the production of hypochlorous acid by human neutrophils (IC50 = 50 nM) and inhibits the formation of NADH bromohydrin (IC50 = 70 nM with 50 µM H2O2 and 10 mM NaBr).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number
532280
Brand Family
Calbiochem®
Synonyms
MPO Inhibitor III, HX1
References
References
Forbes, L. V., et al. 2013. J. Bio. Chem.288, 36636.
Forbes, L. V., et al. 2013. J. Bio. Chem.288, 36636.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
27-January-2015 JSW
Synonyms
MPO Inhibitor III, HX1
Description
A cell-permeable, trifluoromethyl substituted aromatic hydroxamate compound that acts as a highly potent, selective, mixed type, reversible inhibitor of the chlorination activity of myeloperoxidase (MPO; IC50 = 5 nM). Tightly binds within the active site cavity above the heme and blocks the substrate channel. Displays over 300-fold greater selectivity for MPO when tested against a panel of redox enzymes, including lactoperoxidase (IC50 = 6.3 µM) and thyroid peroxidase (IC50 = 1.59 µM). Blocks the production of hypochlorous acid by human neutrophils (IC50 = 50 nM) and inhibits the formation of NADH bromohydrin (IC50 = 70 nM with 50 µM H2O2 and 10 mM NaBr).
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₁₄H₁₀F₆N₄O₃
Purity
≥98% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
+2°C to +8°C
Protect from light
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Forbes, L. V., et al. 2013. J. Bio. Chem.288, 36636.
