Tankyrase1/2 Inhibitor, XAV939-Calbiochem

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一般描述

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 ?M, 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 ?M, respectively)in vitroand prevent the regeneration of zebrafish tail fin (by ~70% at 7 d post-amputation, 5 ?M) after surgical removalin vivo.

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

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