TNKS-IN-1 is a selective and potent tankyrase ( TNKS1 / TNKS2 ) inhibitor with IC50 values of 7.9 nM and 8.7 nM. TNKS-IN-1 induces axin2 accumulation with an EC 50 of 1500 nM. TNKS-IN-1 can antagonize the Wnt signal transduction pathway by stabilizing axin proteins and promoting β-catenin degradation. TNKS-IN-1 can be used for the research of colorectal cancer [1].
In Vitro, TNKS-IN-1 (Compound 3a) (1 h) potently inhibits purified human TNKS1 and TNKS2 with IC50 values of 7.9 nM and 8.7 nM, respectively, and exhibits >10000 nM for PARP1[1]. TNKS-IN-1 (24 h) induces axin2 accumulation in DLD1 cells with an EC50 of 1500 nM, confirming cellular tankyrase inhibition activity[1].
References:
[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019;62(17):7897-7909.
In Vitro, TNKS-IN-1 (Compound 3a) (1 h) potently inhibits purified human TNKS1 and TNKS2 with IC50 values of 7.9 nM and 8.7 nM, respectively, and exhibits >10000 nM for PARP1[1]. TNKS-IN-1 (24 h) induces axin2 accumulation in DLD1 cells with an EC50 of 1500 nM, confirming cellular tankyrase inhibition activity[1].
References:
[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019;62(17):7897-7909.