ML130 (Nodinitib-1) 799264-47-4

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Molecular Weight:

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.

Biological 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.


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.

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Product Categories : NF-κB > NOD1 Inhibitor