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IWR-1-endo
- IWR-1 - endo-IWR-1
- Soluble in DMSO
- MF: C25H19N3O3
- MW: 409.44
Description
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.
More Information
| Parent CAS No. | 1127442-82-3 |
|---|---|
| Chemical Name | rel-4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide |
| MFCD | N.A. |
| Short Description | Wnt/TNKS inhibitor |
References
- S.M. Huang et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-20.
- B. Chen et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
- C. Liu et al. Destruction of a destructor: a new avenue for cancer therapeutics targeting the Wnt pathway. J Mol Cell Biol. 2010 Apr;2(2):70-3.
- Y. Ren et al. Small molecule Wnt inhibitors enhance the efficiency of BMP-4-directed cardiac differentiation of human pluripotent stem cells. J Mol Cell Cardiol. 2011 Sep;51(3):280-7.
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