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    IKK-16 (IKK Inhibitor VII; IKK 16)
    IKK-16 (IKK Inhibitor VII; IKK 16)

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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 #: V0750
    CAS #: 873225-46-8Purity ≥98%

    Description: IKK-16 (also known as IKK Inhibitor VII; IKK-16; IKK16) is a novel, potent and selective IκBα kinase (IKK) inhibitor with potential anti-inflammatory activity. It inhibits IKK-2, IKK complex and IKK-1 with IC50s of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. In addition, IKK-16 has been found to be active at thioglycollate-induced peritonitis model in the mouse. Furthermore, IKK-16 has revealed to be an orally bio-available in rats and mice, and have significant in vivo activity in an acute model of cytokine release.

    References: Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12.

    Related CAS #: 1186195-62-9 (HCl)    873225-46-8 (free base)                           

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    Molecular Weight (MW)483.63
    FormulaC28H29N5OS
    CAS No.873225-46-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 97 mg/mL (200.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL  
    Synonym

    Synonym: IKK 16; IKK Inhibitor VII; IKK-16; IKK16;

    Chemical Name: (4-((4-(benzo[b]thiophen-2-yl)pyrimidin-2-yl)amino)phenyl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone

    InChi Key: BWZJBXAPRCVCKQ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C28H29N5OS/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31)

    SMILES Code: O=C(C1=CC=C(NC2=NC=CC(C3=CC4=CC=CC=C4S3)=N2)C=C1)N5CCC(N6CCCC6)CC5           


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    In Vitro

    In vitro activity: IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker.


    Kinase Assay: IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM. 


    Cell Assay: IKK-16 (IKK Inhibitor VII) inhibited IKK2 by the blockade of IκBα degradation and suppressed TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Moreover, IKK-16 also showed activity in the IFNγ-induced expression of the MHC molecules β2 microglobulin and HLA-DR, but its potency in these assays is 4- to 10-fold weaker than the adhesion molecules assay.

    In VivoIKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis
    Animal modelRat model; thioglycollate-induced peritonitis model in the mouse 
    Formulation & Dosage30 mg/kg; s.c. injection or oral administration
    References

    Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12.


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

      Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12.


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