492002

NOX1 Inhibitor, ML171

The NOX1 Inhibitor, ML171, also referenced under CAS 6631-94-3, controls the biological activity of NOX1.

• Synonyme(s) : NOX1 Inhibitor, ML171, NADPH Oxidase-1 Inhibitor, ML171, 2-APT, 2-acetylphenothiazine
• Formule empirique (notation de Hill): C₁₄H₁₁NOS
• Numéro CAS: 6631-94-3
• Poids moléculaire : 241.31
• Numéro MDL: MFCD00005017
• Code UNSPSC : 41121801
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: dark yellow-orange
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C14H11NOS/c1-9(16)10-6-7-14-12(8-10)15-11-4-2-3-5-13(11)17-14/h2-8,15H,1H3
• Clé InChI: JWGBOHJGWOPYCL-UHFFFAOYSA-N

Description

Description générale

A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC₅₀ = 0.129 µM, and 0.25 µM) in human HT29 and HEK293 cell-based assays, respectively. Unlike most other currently used Nox inhibitors, it only has marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms (IC₅₀ = 5 µM, 3 µM and 5 µM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC₅₀ = 5.5 µM) in HEK293 cell-based assays. It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ~ 100 nM; however, its inhibitory effect is reversed through over-expression of Nox1, thereby suggesting that this compound is highly selective for Nox1, with little effect against Nox2-dependent ROS generation (IC₅₀ >10 µM). Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.

A highly selective, cell-permeable, and reversible 2-acetylphenothiazine that is shown to inhibit NADPH Oxidase-1 (Nox1) (IC₅₀ = 0.129 µM, and 0.25 µM) in human HT29 and HEK293 cell-based assays, respectively. Unlike most other currently used Nox inhibitors, it only has marginal activity on other cellular ROS-producing enzymes and receptors including the other Nox isoforms (IC₅₀ = 5 µM, 3 µM and 5 µM for Nox2, Nox3, and Nox4, respectively) and xanthine oxidase, XO, (IC₅₀ = 5.5 µM) in HEK293 cell-based assays. It is also shown to block Nox1-dependent ROS generation in HEK293 cultures dose-dependently at concentrations up to ~100 nM; however, its inhibitory effect is reversed through over-expression of Nox1, thereby suggesting that this compound is highly selective for Nox1, with little effect against Nox2-dependent ROS generation (IC₅₀ >10 µM). Qualitatively, it displays an inhibitory effect against SrcYF-induced ECM-degrading invadopodia formation in DLD1 Human Colon Cancer Cells.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

Gianni, D., et al. 2010. ACS Chem. Biol.5, 981.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3