1127442-82-3
Chemical Structure
IWR-1
Synonym(s): endo-IWR 1; IWR-1-endo
- CAS 番号: 1127442-82-3
- Formula:C25H19N3O3
- Molecular Weight:409.44
IUPAC Name: 4-((3aR,4S,7R,7aS)-1,3-dioxo-1,3,3a,4,7,7a-hexahydro-2H-4,7-methanoisoindol-2-yl)-N-(quinolin-8-yl)benzamide
InChIKey: ZGSXEXBYLJIOGF-ALFLXDJESA-N
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
Biological Activity: 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].
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IWR-1 | 99.60% | 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. | ||||||||||||||||||||
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IWR-1 (GMP) | IWR-1 (IWR-1-endo) (GMP) is the IWR-1 (HY-12238) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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. | |||||||||||||||||||||
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IWR-1 (Standard) | ≥98% | IWR-1 (Standard) is the analytical standard of IWR-1 (HY-12238). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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.
- [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). [Content Brief]
