Myeloperoxidase Inhibitor-I - CAS 5351-17-7 - Calbiochem

General description

A benzoic acid hydrazide analog that acts as a potent, irreversible, and specific inhibitor of the peroxidation activity of myeloperoxidase (MPO; IC₅₀ = 300 nM). Does not inhibit catalase or glutathione peroxidase activities. Does not affect the production of superoxide by neutrophils. Shown to inhibit H₂O₂-induced apoptosis in HL-60, human leukemia cells.

A benzoic acid hydrazide analog that acts as a potent, specific, and irreversible inhibitor of myeloperoxidase. ABAH is a mechanism-based inhibitor that is oxidized to radical intermediates that, in turn, promote the irreversible inactivation of myeloperoxidase. Reported to inhibit hypochlorous acid (HOCl) production by purified myeloperoxidase (IC₅₀ = 300 nM). Has also been shown to inhibit HOCl production up to 90% in zymosan and phorbol myristate acetate stimulated neutrophils (IC₅₀ = 16 µM and 2.2 µM, respectively). Does not affect superoxide radical production or degranulation of neutrophils and does not inhibit catalase or glutathione peroxidase. Shown to inhibit myeloperoxidase-mediated apoptosis in >90% of ras-expressing fibroblasts and glutathione-depleted, src-transformed cells. Also shown to inhibit apoptosis in H₂O₂-treated HL-60 promyelocytic leukemia cells.

Biochem/physiol Actions

Cell permeable: no

Primary Target
Myeloperoxidase

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 300 nM against myeloperoxidase (MPO)

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Engelmann, I., et al. 2000. Redox Report5, 207.
Wagner, B.A., et al. 2000. J. Biol. Chem.275, 22461.
Burner, U., et al. 1999. J. Biol. Chem.274, 9494.
Kettle, A.J., et al. 1997. Biochem. J.321, 503.
Kettle, A.J., et al. 1995. Biochem. J.308, 559.

Legal Information

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