Myeloperoxidase Inhibitor III, HX1

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).

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.

Cell permeable: yes

Primary Target
MPO

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Forbes, L. V., et al. 2013. J. Bio. Chem.288, 36636.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany