Tankyrase1/2 Inhibitor, XAV939 – Calbiochem

Descrição detalhada : A cell-permeable dihydrothiopyranopyrimidinol that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (Kd = 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 microM, 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 microM, respectively) in vitro and prevent the regeneration of zebrafish tail fin (by ~70% at 7 d post-amputation, 5 microM) after surgical removal in vivo.
Sinónimos : Tankyrase1/2 Inhibitor, XAV939 - Calbiochem; 2-(4-(Trifluoromethyl)phenyl)-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidin-4-ol, Wnt Pathway Inhibitor V, TNKS1/2 Inhibitor I
Fórmula molecula r: C14H11F3N2OS
Armazenamento : -20C
Embalagem : 1X10MG