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Merck

475944

Myeloperoxidase Inhibitor-I

The Myeloperoxidase Inhibitor-I, also referenced under CAS 5351-17-7, controls the biological activity of Myeloperoxidase. This small molecule/inhibitor is primarily used for Inflammation/Immunology applications.

Synonyme(s) :

Myeloperoxidase Inhibitor-I

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A propos de cet article

Formule empirique (notation de Hill) :
C7H9N3O
Numéro CAS:
Poids moléculaire :
151.17
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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description

RTECS - DG2580000

Quality Segment

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

beige

solubility

DMSO: 10 mg/mL, dilute acid: soluble

shipped in

ambient

storage temp.

−20°C

SMILES string

N(N)C(=O)c1ccc(cc1)N

InChI

1S/C7H9N3O/c8-6-3-1-5(2-4-6)7(11)10-9/h1-4H,8-9H2,(H,10,11)

InChI key

WPBZMCGPFHZRHJ-UHFFFAOYSA-N

General description

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

Preparation Note

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

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

Disclaimer

Toxicity: Irritant (B)


Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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