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    NOD-IN-1
    NOD-IN-1

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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 #: V3277
    CAS #: 132819-92-2 Purity ≥98%

    Description: NOD-IN-1 is a novel and potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors with IC50 of 5.74 μM and 6.45 μM for NOD1 and NOD2, respectively. It displayed a balanced inhibitory activity on both targets in the low micromolar range. NOD1 and NOD2 are important members of the pattern recognition receptor family and play a crucial role within the context of innate immunity. However, overactivation of NODs, especially of NOD1, has also been implicated in a number of diseases. Surprisingly, NOD1 remains a virtually unexploited target in this respect. 

    References:  2016 Nov 1;24(21):5221-5234. 


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    Molecular Weight (MW) 343.40
    Formula C18H17NO4S 
    CAS No. 132819-92-2 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 10 mM
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Chemical Name Ethyl 1-tosyl-1H-indole-2-carboxylate
    Synonyms NOD-IN-1; NOD-IN1; NOD-IN 1
    SMILES Code O=C(C(N1S(=O)(C2=CC=C(C)C=C2)=O)=CC3=C1C=CC=C3)OCC


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    In Vitro

    In vitro activity: NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2 with IC50 of 5.74 μM and 6.45 μM, respectively. NOD1 and NOD2 are important members of the pattern recognition receptor family and play a crucial role within the context of innate immunity. However, overactivation of NODs, especially of NOD1, has also been implicated in a number of diseases. Surprisingly, NOD1 remains a virtually unexploited target in this respect. 


    Kinase Assay: NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2 with IC50 of 5.74 μM and 6.45 μM, respectively. 


    Cell Assay: HEK-Blue NOD1 and NOD2 cells (Invivogen) were cultured in DMEM medium (Sigma) with 10 % heat-deactivated FBS (Gibco), 2 mM l-glutamine (Sigma), 50 U/mL penicillin (Sigma), 50 ng/mL streptomycin (Sigma), 4.5 g glucose (Sigma) and 100 μg/mL Normocin (Invivogen) for 2 passages. All subsequent passages were cultured in the medium supplemented with 30 μg/mL Blasticidin (Invivogen) and 100 μg/mL Zeocin (Invivogen). The experiments were carried out on passages 7–12. NOD-IN-1 (compound 4) is potent mixed inhibitor of NOD1 and NOD2, displaying a balanced inhibitory activity on both targets in the low micromolar range. NOD-IN-1 (IC50 (NOD1)=5.74 μM; IC50 (NOD2)=6.45 μM) is identified as the best of the series, possessing NOD1- and NOD2-inhibitory activities in the lower micromolar range. These results show that NOD-IN-1 is 7-fold less potent than Noditinib-1 in terms of NOD1 inhibition and completely devoid of selective activity for NOD1 or NOD2 as opposed to Noditinib-1. NOD-IN-1 exhibits balanced dual activities of less than 10 μM on the two targets. 

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    References  2016 Nov 1;24(21):5221-5234.


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

     

    NOD-IN-1

    Figure 2. Proliferation rates, expressed as metabolic activities, of HEK-Blue cells after 24 h treatment with the synthesized compounds and Noditinib-1 (25 μM).  2016 Nov 1;24(21):5221-5234.

     

    NOD-IN-1

    Figure 3. Effects of synthesized compounds 4–7, 9–12 and Noditinib-1 (1) on the inhibition of C12-iE-DAP-induced NF-κB transcriptional activity.  2016 Nov 1;24(21):5221-5234.

     

    NOD-IN-1

    Figure 4. Inhibition of C12-iE-DAP-induced NF-κB transcriptional activity by compounds 4 (NOD-IN-1) and 39–43.  2016 Nov 1;24(21):5221-5234.

     

    NOD-IN-1

    Figure 5. Effects of compounds 9 and 13–19 on the inhibition of C12-iE-DAP-induced NF-κB transcriptional activity.  2016 Nov 1;24(21):5221-5234.

     

    NOD-IN-1

    Figure 6. Inhibition of C12-iE-DAP-induced NF-κB transcriptional activity by compounds 12, 33–38, 44 and 45.  2016 Nov 1;24(21):5221-5234.

     

    NOD-IN-1

    Figure 1. The design of novel NOD1 inhibitors based on structures of 1 (Noditinib-1) and 2.  2016 Nov 1;24(21):5221-5234.


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