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XAV939
- Development stage
- Preclinical
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- In Vitro Use
01
Overview
XAV939 is a potent, selective small molecule inhibitor of **tankyrase 1 (TNKS1) and tankyrase 2 (TNKS2)**, a subclass of poly (ADP-ribose) polymerases (PARPs)[1][4][5][8]. It exerts its activity by stabilizing axin, a concentration-limiting component of the beta-catenin destruction complex, resulting in **degradation of β-catenin and inhibition of the canonical Wnt/β-catenin pathway**[1][4][5][8]. XAV939 suppresses the proliferation and migration of multiple cancer cell lines (including colon, lung, neuroblastoma, and breast cancers) by antagonizing abnormal Wnt signaling[3][5][7][9]. The compound is widely used in research for stem cell differentiation, particularly in cardiomyocyte and neuronal differentiation protocols, and as a chemical probe to investigate the Wnt/β-catenin pathway[1][5]. It is for research use only and not approved for human therapeutic or diagnostic use[2].
- Other names
- XAV939XAV-939XAV 939NVP-XAV939NVP-XAV-939NVP-XAV 939XAV dCS-300CS300CS 300
02
Targets
TNKS (Poly(ADP-ribose) Polymerase 5a)TNKS2 (Tankyrase 2)CTNNB1 (Beta-catenin)
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