IWR-1

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 Specifications

CAS Number

[1127442-82-3]

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) .