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Wnt&Beta catenin

IWR-1-endo (1127442-82-3)

Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM.

Not Intended for Therapeutic Use. For research use only.

CAS: 1127442-82-3 Category

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

Product Name IWR-1
Synonyms IWR-1; IWR 1; IWR1; IWR-1-endo.
Chemical Names 4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-benzamide
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1127442-82-3
Molecular Formula C25H19N3O3
Molecular Weight 409.44
Monoisotopic Mass 409.143 g/mol
MDL number N/A
InChIKey ZGSXEXBYLJIOGF-UHFFFAOYSA-N
InChi Code InChI=1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)
SMILES O=C(NC1=C2N=CC=CC2=CC=C1)C3=CC=C(N(C(C4C(C5)C=CC5C64)=O)C6=O)C=C3
Form Powder
Color N/A
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

 


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RIDADR NONH for all modes of transport

References:

  • Chen, B., Dodge, M.E., Tang, W., et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer Nature Chemical Biology 5(2), 100-107 (2009).
  • Lu, J., Ma, Z., Hsieh, J.C., et al. Structure-activity relationship studies of small-molecule inhibitors of Wnt response Bioorganic & Medicinal Chemistry Letters 19, 3825-3827 (2009).
  • Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Chen et al.Nature Chem.Biol., 2008;5:100
  • M. Huang et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-20.
  • 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.
  • 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.

1 review for IWR-1-endo (1127442-82-3)

  1. Cofttek

    Never had such good experience before,The IWR-1-endo (1127442-82-3) is high purity,also customer service is pretty nice !gotta try!!

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