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    ML130 (Nodinitib-1)
    ML130 (Nodinitib-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 #: V0747
    CAS #: 799264-47-4Purity ≥98%

    Description: ML130 (also known as Nodinitib-1; ML-130; CID1088438; CID-1088438) is a novel, potent and selective inhibitor of NOD1 (nucleotide-binding oligomerization domain containing 1) with potential anti-inflammatory activity. It inhibits NOD1 with an IC50 of 0.56 μM. It acts by inhibiting NF-κB activation and exhibiting 36-fold selectivity for NOD1 over NOD2. ML130 selectively inhibits NOD1-dependent activation of NF-κB and MAPK signaling and also inhibits NOD1-induced IL-8 production in MCF-7 cells without affecting viability. In ex vivo dendritic cell culture, 15 μM noditinib-1 reduced cell-surface expression of CD83, CD86, and HLA-DR and inhibited expression of IL-1β, IL-6, and TNF-α.

    References: Chem Biol. 2011 Jul 29;18(7):825-32; ACS Med Chem Lett. 2011 Oct 13;2(10):780-785

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    Molecular Weight (MW)287.34
    FormulaC14H13N3O2S
    CAS No.799264-47-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 57 mg/mL (198.4 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL (7.0 mM)
    SMILESNC1=NC2=CC=CC=C2N1S(=O)(C3=CC=C(C)C=C3)=O
    SynonymsNodinitib-1; ML130; ML 130; CID1088438; ML-130; CID-1088438; CID 1088438; Nodinitib 1; Nodinitib1;  

    Chemical Name: 1-(4-methylphenyl)sulfonylbenzimidazol-2-amine

    InChi Key: SRFABRWQVPCPRG-UHFFFAOYSA-N

    InChi Code: InChI=1S/C14H13N3O2S/c1-10-6-8-11(9-7-10)20(18,19)17-13-5-3-2-4-12(13)16-14(17)15/h2-9H,1H3,(H2,15,16)

    SMILES Code: NC1=NC2=CC=CC=C2N1S(=O)(C3=CC=C(C)C=C3)=OInChI=1S/C14H13N3O2S/c1-10-6-8-11(9-7-10)20(18,19)17-13-5-3-2-4-12(13)16-14(17)15/h2-9H,1H3,(H2,15,16)           


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    In Vitro

    In vitro activity: ML130 has shown selective inhibition of NOD1-induced NF-κB activation in HEK293 cells with no cytotoxicity and is selected as a probe candidate molecule. ML130 is also confirmed in secondary assays by selectively inhibiting NOD1-dependent IL-8 secretion and also selectively inhibiting the NOD1-dependent pathway to NF-κB activation. In another research, ML130 is proved to cause conformational changes of NOD1 in vitro and alter NOD1 subcellular targeting in cells, providing chemical probes for interrogating mechanisms regulating NOD1 activity and tools for exploring the roles of NOD1 in various infectious and inflammatory diseases


    Kinase Assay: Day 1 Procedure 1) Harvest HEK-293-T NFKB-Luc at 100% confluency at 100% confluency. 2) Add NOD assay media with Multidrop. 3) Spin down plates at 1000 rpm for 1 min in centrifuge. 4) Serial compound dilutions. 5) Add gamma-tri-DAP to cell suspension at 0.75 ug/mL. 6) Seed 13000 cells/well in 4 uL/well to full plate HEK-293-T NFKB-Luc to TC-treated plate. 7) Spin down plates 500 RPM for 5 min on centrifuge. 8) Lid Plates. Sandwich 4 plates between 2 lidded 384 plates filled with H2O. 9) Wrap plates securely in single layer of Plastic Wrap. 10) Incubate overnight (14 hours) in 37 ℃ and 5% CO2 incubator. Day 2 Procedure 1) Add 3 ul/well of SteadyGlo solution with Multidrop. 2) Shake plates on a plate shaker for 20 min. 3) Spin plates 1000 RPM for 1 min using centrifuge. 4) Read luminescence.IC50 values are calculated using GraphPad Prism 5.0.The average Z' for the screen is 0.6, the signal to background is 11.1, signal to noise is 78.6 and signal to window is 6.0.


    Cell Assay: Hepatic toxicity of compounds is determined with Fa2N-4 immortalized human hepatocytes using the ATP-lite 1-step assay. Fa2N-4 cells are seeded at 50,000 cells/well, and incubated with a range of concentrations of the test compound (0.01 µM-50 µM) in MFE support medium for 24 h at 37 ℃, 5% CO2. At the end of the experiment D-luciferin and luciferase are added. The emitted luminescent signal produced as a result of the reaction with cellular ATP is captured on the Infinite M200 plate reader. The concentration of each compound that killed 50% of the cells (LC50) is calculated by non-linear regression analysis using a log (inhibitior) vs response equation with a variable slope, using the statistic software package Prism4.

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    References

    Chem Biol. 2011 Jul 29;18(7):825-32; ACS Med Chem Lett. 2011 Oct 13;2(10):780-785


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

     

    ML130 (Nodinitib-1)

    Profiling 2-aminobenzimidazole (ML130)derivatives for pathway selectivity. Chem Biol. 2011 Jul 29;18(7):825-32.
     

    ML130 (Nodinitib-1)

    CID-1088438 (ML130 analog) specifically inhibits NOD1-dependent signaling pathways. Chem Biol. 2011 Jul 29;18(7):825-32.
     

    ML130 (Nodinitib-1)

    Analysis of mechanisms of chemical inhibitors of NOD1. Chem Biol. 2011 Jul 29;18(7):825-32.


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