IWR-1

• Description:

  IWR-1 (IWR-1-endo) is a tankyrase inhibitor targeting Wnt/β-catenin (IC50 = 180 nM) . IWR-1 compromises critical steps of the canonical Wnt signaling, namely translocation of β-catenin to the nucleus and subsequent TCF/LEF activation and expression of Wnt/β-catenin downstream targets. IWR-1 promotes β-catenin phosphorylation by promoting stability of Axin-scaffolded destruction complexes. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis[1][2][4].

• Product Name Alternative:

  Endo-IWR 1; IWR-1-endo

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Organoid; Wnt

• Type:

  Reference compound

• Related Pathways:

  Stem Cell/Wnt

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer; Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/IWR-1.html

• Purity:

  99.60

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)

• Smiles:

  O=C (NC1=C2N=CC=CC2=CC=C1) C3=CC=C (N (C ([C@]4 ([H]) [C@] (C5) ([H]) C=C[C@]5 ([H]) [C@]64[H]) =O) C6=O) C=C3

• Molecular Formula:

  C25H19N3O3

• Molecular Weight:

  409.44

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Sara R. Martins-Neves, et al., IWR-1, a tankyrase inhibitor, attenuates Wnt/β-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of a subcutaneous human osteosarcoma xenograft, Cancer Letters, Volume 414, 2018, Pages 1-15, ISSN 0304-3835. |[2]Lee SC, et al., IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. Oncotarget. 2015 Sep 29;6 (29) :27146-59.|[3]Wang, W. M., et al., IWR-1 attenuates the promotional effect of IL-36γ in a mouse model of psoriasis. BMC immunology, 25 (1), 78.|[4]Chen, B., Dodge, M.E., Tang, W., et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat. Chem. Biol. 5 (2), 100-107 (2009) .

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  1127442-82-3