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ML130 (Nodinitib-1) (Synonyms: CID1088438, ML130)

Catalog No.GC16641

ML130 (Nodinitib-1) (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.

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ML130 (Nodinitib-1) Chemical Structure

Cas No.: 799264-47-4

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10mM (in 1mL DMSO)
$50.00
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5mg
$45.00
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10mg
$63.00
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25mg
$113.00
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50mg
$180.00
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100mg
$315.00
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Sample solution is provided at 25 µL, 10mM.

Description of ML130 (Nodinitib-1)

Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an IC50 of 0.56 μM.

Nodinitib-1 selectively inhibits IL-8 production induced by NOD1 ligand. Nodinitib-1 also inhibits γ-tri-DAP-induced expression of the prototypical NF-κB target gene IκBα at the mRNA level. Nodinitib-1 inhibits γ-tri-DAP-dependent activation of NF-κB (IκBα phosphorylation and degradation) and MAPK (p38 phosphorylation) signalings, without affecting Akt survival pathway. Nodinitib-1 selectively inhibits responses of primary dendritic cells to NOD1 ligand. Nodinitib-1 reduces cell surface expression of co-stimulatory molecules CD83, CD86 and HLA-DR and also inhibits expression of IL-1β, IL-6 and TNFα elicited by γ-tri-DAP (but not by LPS), without causing cytoxicity[1]. Nodinitib-1 is identified as NOD1-selective molecules from an HTS campaign involving ~290,000 compounds. Nodinitib-1 inhibits γ-tri-DAP-stimulated luciferase production in HEK 293T cells, which has endogenous NOD1 levels at submicromolar concentration as determined in a NF-κB-linked reporter assay[2].

References:
[1]. Correa RG, et al. Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors. Chem Biol. 2011 Jul 29;18(7):825-32.
[2]. Hershberger PM, et al. Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway. Beilstein J Org Chem. 2013 May 8;9:900-7.

Protocol of ML130 (Nodinitib-1)

Cell experiment:

RAW264.7 cells are treated with 5 μM of CID-1088438 or CID-44229067 alone, or also infected with S. typhimurium at multiplicity of infection (MOI) of 20 and 200 bacteria per mammalian cell. Cell viability is analyzed two hours after Salmonella infection by measuring ATP levels. Percentage viability is calculated according to the ATP levels of respective non-infected cells. Values presented are averages of two replicates (+ SEM)[1].

References:

[1]. Correa RG, et al. Discovery and characterization of 2-aminobenzimidazole derivatives as selective NOD1 inhibitors. Chem Biol. 2011 Jul 29;18(7):825-32.
[2]. Hershberger PM, et al. Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway. Beilstein J Org Chem. 2013 May 8;9:900-7.

Chemical Properties of ML130 (Nodinitib-1)

Cas No. 799264-47-4 SDF
Synonyms CID1088438, ML130
Chemical Name 1-(4-methylphenyl)sulfonylbenzimidazol-2-amine
Canonical SMILES CC1=CC=C(C=C1)S(=O)(=O)N2C3=CC=CC=C3N=C2N
Formula C14H13N3O2S M.Wt 287.34
Solubility DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:8): 0.11 mg/ml,DMSO: 13 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ML130 (Nodinitib-1)

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1 mg 5 mg 10 mg
1 mM 3.4802 mL 17.401 mL 34.802 mL
5 mM 0.696 mL 3.4802 mL 6.9604 mL
10 mM 0.348 mL 1.7401 mL 3.4802 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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