TDI-012804 is a TNKS2 inhibitor that selectively inhibits intracellular endogenous TNKS2 protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids ( EC 50 of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids [1].
References:
[1]. Jill Zimmerman, et al. A potent and selective TNKS2 inhibitor for tumor-selective WNT suppression. bioRxiv.2025 Mar 7:2025.03.04.641305.
References:
[1]. Jill Zimmerman, et al. A potent and selective TNKS2 inhibitor for tumor-selective WNT suppression. bioRxiv.2025 Mar 7:2025.03.04.641305.
















