573109

STAT3 Inhibitor VIII, 5,15-DPP

The STAT3 Inhibitor VIII, 5,15-DPP, also referenced under CAS 22112-89-6, controls the biological activity of STAT3.

• Synonyme(s) : STAT3 Inhibitor VIII, 5,15-DPP, 5,15-Diphenylporphyrin
• Formule empirique (notation de Hill): C₃₂H₂₂N₄
• Numéro CAS: 22112-89-6
• Poids moléculaire : 462.54
• Numéro MDL: MFCD08276335
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥90% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: deep blue to deep purple
• Solubilité: DMSO: <1 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

A cell-permeable porphyrin compound that binds STAT3 (K_D = 880 nM by SPR) and prevents STAT3 SH2 domain-mediated ligand binding (IC₅₀ = 280 nM) and dimerization (~60% inhibition at 50 µM in HEK293), while exhibiting much reduced activity against STAT1 ligand binding (IC₅₀ = 10 µM) and no activity againt Grb2 ligand binding even at concentrations as high as 20 µM. One day 5,15-DPP pre-treatment (50 µM) of MDA-MB-468 cultures is shown to greatly inhibit IL-6-induced STAT3, but not STAT1/5a/5b, nuclear translocation (by >90%) and nuclear STAT3 c-myc promoter binding activity, resulting in a more than 90% reduction in cellular c-myc protein level.

A cell-permeable porphyrin compound that directly binds to STAT3, prevents STAT3 dimerization and acts as a STAT3-SH2 domain antagonist with selectivity over STAT1 and Grb2 (IC₅₀ = 0.28, 10 and >20 µM, respectively). Shown to preferentially suppress STAT3 nuclear translocation and subsequent DNA binding in MDA-MB-468 cells with negligible effect on STAT1, STAT5a and STAT5b; further, reduce c-myc promoter binding and c-myc protein expression in IL-6 induced HEK-293-STAT3 cells. Does neither affect JAK kinase activity nor lower the expression or the phosphorylation levels of STAT3.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Uehara, Y., et al. 2009. Biochem. Biophys. Res. Commun.380, 627.

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
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable