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.
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(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.
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Choose Selective NOD1 Inhibitors
|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.|
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. 
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.
|In vitro||DMSO||57 mg/mL (198.37 mM)|
|Ethanol||2 mg/mL (6.96 mM)|
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