ML130 (Nodinitib-1)

Catalog No.S2863

ML130 (Nodinitib-1) Chemical Structure

Molecular Weight(MW): 287.34

ML130 (Nodinitib-1) is a potent and selective inhibitor of NOD1 with IC50 of 0.56 μM, inhibits NF-κB activation, exhibits 36-fold selectivity over NOD2.

Size Price Stock Quantity  
In DMSO USD 100 In stock
USD 90 In stock
USD 110 In stock
USD 170 In stock
USD 270 In stock
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Cited by 5 Publications

2 Customer Reviews

  • (E) Gentamicin protection assay performed as in (B) with healthy control MDM (n=4). Quantification of S. typhimurium-CFU after inhibition of NOD1 with ML-130 and MDP pre-stimulation.

    Gut, 2016, 66(6):1060-1073. ML130 (Nodinitib-1) purchased from Selleck.

    Effect of ML130 on E. coli-induced NF- B activation in neutrophils. (A) Freshlyisolated neutrophils were pretreated with or without ML130 for 2 h, followed byexposure to live E. coli for 30 min. Nuclear translocation of NF- B was assessedby Western blot analysis. (B) The densitometric analysis of Western blots. Data(mean ± SEM of 4 heifers) are presented as fold changes over untreated samples afternormalisation to -actin within the same sample. One of 3 independent experimentsis shown. ** P < 0.01 and *** P < 0.001.

    Vet Immunol Immunopathol, 2015, 168(1-2):68-76. ML130 (Nodinitib-1) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description ML130 (Nodinitib-1) is a potent and selective inhibitor of NOD1 with IC50 of 0.56 μM, inhibits NF-κB activation, exhibits 36-fold selectivity over NOD2.
Targets
NOD1 [1]
()
0.56 μM
In vitro

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. [1] 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. [2]

Assay
Methods Test Index PMID
Western blot
p-NF-κB / NF-κB / TNFα; 

PubMed: 22450316     


HAPI cells were treated with ML130 (a Nod1 inhibitor) for 14 hour, followed by LPS. HAPI cells were collected, and pNF-κB was examined using Western blots. ML130 reduced the expression of pNF-κB (C). In the same sample, the expression of TNFα (D) was suppressed by ML130. *p<0.05, **p<0.01 vs vehicle.

22450316

Protocol

Kinase Assay:[1]
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NOD1 Dose Response 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 Research:[1]
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  • Cell lines: Fa2N-4 cells
  • Concentrations: 0.01 μM-50 μM
  • Incubation Time: 24 h
  • Method: 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (198.37 mM)
Ethanol 2 mg/mL (6.96 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 287.34
Formula

C14H13N3O2S

CAS No. 799264-47-4
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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NOD1 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID