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    InvivoChem Cat #: V1351
    CAS #: 1127442-82-3Purity ≥98%

    Description: IWR-1-endo (also known as IWR 1-endo; IWR1; IWR-1) is a potent tankyrase inhibitor of the Wnt pathway with potential antitumor activity. It inhibits tankyrase with an IC50 of 180 nM in L-cells expressing Wnt3A.  IWR-1-endo is able to induce Axin2 protein levels and promote 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.

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    Molecular Weight (MW)409.44
    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
    Other info

    Chemical Name: 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


    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 Code: O=C(NC1=C2N=CC=CC2=CC=C1)C3=CC=C(N(C(C4C(C5)C=CC5C64)=O)C6=O)C=C3


    IWR-1; IWR-1 endo; IWR 1; IWR 1-endo; IWR1; IWR-1-endo; 

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    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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    Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7; Int J Biol Sci. 2013 Nov 28;9(10):1108-20.

    These protocols are for reference only. InvivoChem does not independently validate these methods.







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