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Biological Activity:
Tankyrase (TNKS) inhibitor, with IC50 values to be 11 and 4 nM for TNKS1 and TNKS2 respectively; inhibiting Wnt / β-catenin signaling.
References:
SM Huang et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling. Nature 2009, 461, 614-620. [online]
R Nusse. Wnt signaling and stem cell control. Cell Res. 2008, 18, 523-527. [online]
RT Peterson, Propping up a destructive regime. Nature 2009, 461, 599–600. [online]
EM Adler. Inhibiting Wnt signaling. Sci. Signal. 2009, 2(91), ec326. [online]
CE Meacham et al. In vivo RNAi screening identifies regulators of actin dynamics as key determinants of lymphoma progression. Nature Gen. 2009, 41(10), 1131-1137. [online]
Chemical Name: 2-[4-(trifluoromethyl)phenyl]-7,8-dihydro-5H-thiino[4,3-d]pyrimidin-4-ol
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