product name IWR-1-endo
Description: IWR-1-endo, also known as IWR-1, is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, it induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. IWR-1-endo binds 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.
References: Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7; Int J Biol Sci. 2013 Nov 28;9(10):1108-20.
409.44
Formula
C25H19N3O3
CAS No.
1127442-82-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 30 mg/mL (73.27 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Although both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. Kinase Assay: IWR-1(IWR-1-endo) is a novel small-molecule inhibitor of Wnt signaling by stabilizing the Axin destruction complex with an EC50 of 0.2 uM Cell Assay: During NSPC differentiation, MIF increased the activity of β-galactosidase that responds to Wnt/β-catenin signaling. Wnt1 and β-catenin proteins were also up-regulated with MIF stimulation. Moreover, the expression of DCX and Tuj 1 was inhibited significantly by IWR-1. FSH treatment increased CYP19A1, CCND2, CTNNB1, AXIN2 and FZD6 mRNAs and the stimulatory effect on CYP19A1 mRNA was reduced by IWR-1. |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7; Int J Biol Sci. 2013 Nov 28;9(10):1108-20. |
