XAV-939 (284028-89-3) is a tankyrase inhibitor (IC50=11 and 4 nM for TNKS1 and 2 respectively). Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of actin.1 XAV-939 robustly induces cardiomyogenesis of stem cells.2 Cell permeable
A tankyrase (TNKS) inhibitor that antagonizes Wnt signaling via stimulation of β-catenin degradation and stabilization of axin. It inhibits proliferation of the μ-catenin-dependent colon carcinoma cell line DLD-1.
XAV939 has been used in the inhibition
- of tankyrase in neuroblastoma cell lines
- of diphtheria toxin-like ADP-ribosyltransferases (ARTD) in medulloblastoma cells
- of wnt signalling in human induced pluripotent stem cells (hiPSCs)
ChEBI: XAV939 is a thiopyranopyrimidine in which a 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine skeleton is substituted at C-4 by a hydroxy group and at C-2 by a para-(trifluoromethyl)phenyl group. It has a role as a tankyrase inhibitor. It is a thiopyranopyrimidine and a member of (trifluoromethyl)benzenes.
XAV939 is a cell-permeable dihydrothiopyranopyrimidinol, which elicits anti-tumor functionality against colon, lung, breast and liver cancer. It binds to catalytic poly-ADP-ribose polymerase (PARP) domain of the tankyrase enzyme resulting in β-catenin destruction. It also inhibits tankyrase in neuroblastoma promoting apoptosis in tumor cells.
[1] SHIH-MIN A. HUANG. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling[J]. Nature, 2009, 461 7264: 614-620. DOI:
10.1038/nature08356[2] HANMIN WANG Charles C H Jijun Hao. Cardiac Induction of Embryonic Stem Cells by a Small Molecule Inhibitor of Wnt/β-Catenin Signaling[J]. ACS Chemical Biology, 2010, 6 2: 192-197. DOI:
10.1021/cb100323z
