5.32280

Myeloperoxidase Inhibitor III, HX1

• Synonym(s): Myeloperoxidase Inhibitor III, HX1, MPO Inhibitor III, HX1
• Empirical Formula (Hill Notation): C₁₄H₁₀F₆N₄O₃
• CAS Number: 1520083-61-7
• Molecular Weight: 396.24
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General 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).

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MPO

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

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable