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    IWP-L6
    IWP-L6

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1356
    CAS #: 1427782-89-5Purity ≥98%

    Description: IWP-L6 (IWPL6; IWPL-6; Porcn Inhibitor III ) is an inhibitor of Porcn (EC50 = 0.5 nM), which is also known as Porcupine and is an enzyme catalyzing the palmitoylation of Wnt proteins. 

    References: J Med Chem. 2013 Mar 28;56(6):2700-4.

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    Molecular Weight (MW)472.58
    FormulaC25H20N4O2S2 
    CAS No.1427782-89-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 25 mg/mL (52.9 mM)          
    Water: <1 mg/mL
    Ethanol: <1 mg/mL 
    Other info

    Chemical Name: N-(5-phenyl-2-pyridinyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide

    InChi Key: QESQGTFWEQMCMH-UHFFFAOYSA-N

    InChi Code: InChI=1S/C25H20N4O2S2/c30-22(28-21-12-11-18(15-26-21)17-7-3-1-4-8-17)16-33-25-27-20-13-14-32-23(20)24(31)29(25)19-9-5-2-6-10-19/h1-12,15H,13-14,16H2,(H,26,28,30)

    SMILES Code: O=C(NC1=NC=C(C2=CC=CC=C2)C=C1)CSC3=NC(CCS4)=C4C(N3C5=CC=CC=C5)=O

    Synonyms

    IWP-L6; PORCN Inhibitor III; Wnt Pathway Inhibitor XIX; IWP L6; IWPL6; Porcn Inhibitor III 


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    In Vitro

    In vitro activity: IWP-L6 blocks the phosphorylation of the cytoplasmic Wnt pathway effector Dvl2 in HEK293 cells. In cultured embryonic kidneys, IWP-L6 also inhibits Wnt mediated branching morphogenesis by reversibly blocking Wnt signaling.

    In VivoIWP-L6 is stable in human plasma over 24 h, while rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions. In embryonic zebrafish, IWP-L6 effectively inhibits posterior axis formation, a Wnt/β-catenin dependent developmental process. IWP-L6 (Porcn Inhibitor III) is stable in human plasma over 24 h, it was rapidly metabolized in rat plasma (t1/2 = 190 min), murine plasma (t1/2 = 2 min), and the murine liver S9 fractions (t1/2 = 26 min). The major metabolites are the amide cleavage products. Similar species-dependent metabolitic profiles due to the involvement of carboxylesterase (CES) have been reported with other drug candidates. Despite its modest metabolic stability in mouse-derived plasma, IWP-L6 was highly active in zebrafish. IWP-L6 exhibited more potent activity
    Animal modelRats
    Formulation & Dosage
    References

    J Med Chem. 2013 Mar 28;56(6):2700-4.


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

    IWP-L6

    IWP-L6 (27) blocks the phosphorylation of the cytoplasmic Wnt pathway effector Dvl2. J Med Chem. 2013 Mar 28;56(6):2700-4.
     

    IWP-L6


    Inhibition of the regeneration of tailfin of juvenile zebrafish. J Med Chem. 2013 Mar 28;56(6):2700-4.


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