IWR-1-endo (1127442-82-3) Description
IWR-1, also known as IWR-1-endo, is a an inhibitor of the Wnt signaling cascade through inhibiting TNKSs, binding only to the adenosine-binding site. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. IWR-1 inhibits cell proliferation and EMT even in the presence of TNF-α-induced cancer cell stimulation. IWR-1 also significantly suppressed cell migration, invasion, and matrix metalloproteinase activities of CRC cell lines. IWR-1 provides EMT reversal effects by directly suppressing survivin expression.
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.
IWR-1-endo (1127442-82-3) Specifications
|Synonyms||IWR-1; IWR 1; IWR1; IWR-1-endo.|
|Purity||>98% (or refer to the Certificate of Analysis)|
|Monoisotopic Mass||409.143 g/mol|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||Wnt/β-catenin signaling inhibitor; axin stabilizer|