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    A-205804
    A-205804

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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 #: V1598
    CAS #: 251992-66-2Purity ≥98%

    Description: A-205804 (A205804; A 205804) is a novel selective inhibitor of E-selectin and intercellular adhesion molecule-1 (ICAM-1) expression (IC50 = 20 nM and 25 nM) with potential anticancer activity. ICAM1 is a protein associated with diseases such as Malaria and Hepatocellular Carcinoma. In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations.

    References: J Med Chem. 2001 Oct 11;44(21):3469-87; J Med Chem. 2001 Mar 15;44(6):988-1002.

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    Molecular Weight (MW)300.4
    FormulaC15H12N2OS2
    CAS No.251992-66-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (199.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 4-[(4-Methylphenyl)thio]thieno[2,3-c]pyridine-2-carboxamide

    InChi Key: QQGWEXFLMJGCAL-UHFFFAOYSA-N

    InChi Code: 1S/C15H12N2OS2/c1-9-2-4-10(5-3-9)19-13-7-17-8-14-11(13)6-12(20-14)15(16)18/h2-8H,1H3,(H2,16,18)

    SMILES Code: CC1=CC=C(SC2=C3C=C(SC3=CN=C2)C(N)=O)C=C1           

    Synonyms

    A205804; A-205804; A 205804 


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    In Vitro

    In vitro activity: A-205804 selectively inhibits the surface expression of the cell adhesion molecules ICAM-1 and E-selectin in human endothelial cells. A-205804 inhibites the IL-1β-induced expression of E-selectin (IC50 = 20 nM) and ICAM-1 (IC50 = 10 nM) with essentially the same level of potency as that for TNFα-induced expression. For reasons which are unclear, the ability of A-205804 to inhibit PMA-induced E-selectin expression is significantly reduced (IC50 > 1000 nM), but A-205804 is a potent inhibitor of ICAM-1 expression (IC50 = 40 nM) using this protein-kinase C-activating agent.


    Cell Assay:  In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations. Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs).

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    References

    J Med Chem. 2001 Oct 11;44(21):3469-87; J Med Chem. 2001 Mar 15;44(6):988-1002.


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

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