Catalog No.: PC-24241Not For Human Use, Lab Use Only.
TDI-012804 is a potent and selective Tankyrase 2 (TNKS2) inhibitor with IC50 of 3.46 nM in in vitro PARylation assays, has 25-fold selectivity over TNKS1, suppresses WNT signaling in TNKS depleted cells.
TDI-012804 is a potent and selective Tankyrase 2 (TNKS2) inhibitor with IC50 of 3.46 nM in in vitro PARylation assays, has 25-fold selectivity over TNKS1, suppresses WNT signaling in TNKS depleted cells.
TDI-012804 is potent (EC50 <100nM) and shows TNKS2-selectivity against in TNKS1 isogenic DLD1 cells using an integrated TOP-Flash reporter.
TDI-012804 shows no inhibition of related PARP family enzymes (PARP1, PARP2, and PARP3).
Mutation of L1136 to tyrosine (L1136Y) significantly reduces the potency of TDI-012804 against TNKS2 but has no effect on the activity of XAV939.
TDI-012804 increases AXIN1 protein in TNKS1KO and TNKS1KO/TNKS2WT cells, but not in TNKS1WT or TNKS1KO/TNKS2L1136Y cells.
TDI-012804 is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids, compared to Tnks1WT lines.
