Small-molecule inhibitor of the Wnt/β-catenin pathway (IC50 value 0.18 μM), strongly inhibiting TNKS1 and TNKS2 in biochemical assays, and targeting the acyltransferase Porcupine (Porcn) without inducing Porcn destruction or mislocalization. IWR-1-endo significantly stabilized endogenous TNKS1, TNKS2 and axin 2 by inhibition of auto-PARsylation of TNKS in vivo and independent of the PARsylation activity of PARP1/2. Furthermore, IWR-1 increased expression of genes commonly expressed in cardiac mesoderm/progenitor cell and significantly improved cardiac differentiation when introduced after the application of BMP-4.

KEYWORDS: IWR-1-endo | Supplier | Wnt/TNKS inhibitor | IWR-1 | IWR1 | CAS [1127442-82-3] | DNA-RNA | TNKS1 | TNKS2 | Tankyrase | Inhibitor | catenin | parp | parsylation | axin | cardiac | differentiation | Porcupine | Porcn