575545

XAV939

≥97% (HPLC), solid, Tankyrase1/2 inhibitor, Calbiochem

• Synonyme(s) : Tankyrase1/2 Inhibitor, XAV939, 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V, TNKS1/2 Inhibitor I
• Formule empirique (notation de Hill): C₁₄H₁₁F₃N₂OS
• Poids moléculaire : 312.31
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.54

Propriétés

• product name: Tankyrase1/2 Inhibitor, XAV939, The Tankyrase1/2 Inhibitor, XAV939 controls the biological activity of Tankyrase1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 25 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A cell-permeable dihydrothiopyranopyrimidinol that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (K_d = 99 and 93 nM, respectively) and potently inhibits their PARsylation (poly ADP-ribosylation) activity (IC₅₀ = 11 and 4 nM, respectively), while exhibiting much lower activity against PARP1 and PARP2 (IC₅₀ = 2.194 and 0.114 µM, respectively). TNKS, but not PARP1/2, function knockdown by siRNA or XAV939 treatment suppresses cellular axin1/2 PARsylation and ubiquitination/proteasomal degradation, resulting in axin build-up, β-catenin destruction, and blockage of Wnt signaling. XAV939 is shown to inhibit the growth of β-catenin-dependent DLD-1, but not that of β-catenin-independent RKO, cells (by >95% vs. no effect at 3.3 µM, respectively) in vitro and prevent the regeneration of zebrafish tail fin (by ~70% at 7 d post-amputation, 5 µM) after surgical removal in vivo.

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

Huang, S.M., et al. 2009. Nature461, 614.

Informations légales

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

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• 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