xav-939

Description

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

The Uses of xav-939

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.

The Uses of xav-939

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)

What are the applications of Application

XAV939 is a potent inhibitor of beta-catenin, TNKS1, and TNKS2

Definition

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.

Biochem/physiol Actions

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.

Storage

Room temperature

References

1) Huang?et al. (2009),?Tankyrase inhibition stabilizes axin and antagonizes Wnt signaling; Nature,?46?614 2) Wang?et al. (2011),?Cardiac induction of embryonic stem cells by a small molecule inhibitor of Wnt/β-catenin signaling; Chem. Biol.,?6?192