Home NF-κB NOD inhibitor Nodinitib-1 (ML130) For research use only.

Nodinitib-1 (ML130)

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

Nodinitib-1 (ML130) Chemical Structure

Nodinitib-1 (ML130) Chemical Structure

CAS: 799264-47-4

Selleck's Nodinitib-1 (ML130) has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S286301 DMSO] 57 mg/mL] false] Ethanol] 2 mg/mL] false] Water] Insoluble] false Purity: 99.87%
99.87

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Biological Activity

Description Nodinitib-1(ML130) 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
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]
Kinase Assay 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
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-NF-κB / NF-κB / TNFα 22450316

Chemical Information & Solubility

Molecular Weight 287.34 Formula

C14H13N3O2S
CAS No. 799264-47-4 SDF Download Nodinitib-1 (ML130) SDF
Smiles CC1=CC=C(C=C1)S(=O)(=O)N2C3=CC=CC=C3N=C2N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (198.37 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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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.

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