CRID3 sodium salt

Biological Activity

Potent NLRP3 inflammasome inhibitor; closes the active conformation of NLRP3 to the inactive state. Directly interacts with the Walker B motif within the NLRP3 NACHT domain. Inhibits IL-1β, IL-18 and IL-1α production (IC₅₀ values are 7.2, 10.3 and 12-18 nM, respectively). Selective for NLRP3 over NLRC4 inflammasome and Toll-like receptor signaling. Reduces severity of experimental autoimmune encephalomyelitis, skin inflammation and airway inflammation in mice. Also glutathione S-transferase omega 1 inhibitor. Orally bioavailable.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases.
   Coll et al.
   Nat.Med., 2015;21:248
2. Inflammasome inhibition prevents a-synuclein pathology and dopaminergic neurodegeneration in mice.
   Gordon et al.
   Sci.Transl.Med., 2018;10:eaah4066
3. MCC950 closes the active conformation of NLRP3 to an inactive state.
   Tapia-Abellán et al.
   Nat.Chem.Biol., 2019;15:560
4. MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition.
   Coll et al.
   Nat.Chem.Biol., 2019;15:556
5. Glutathione S-transferase omega 1-1 is a target of cytokine release inhibitory drugs and may be responsible for their effect on interleukin-1β posttranslational processing.
   Laliberte et al.
   J.Biol.Chem., 2003;278:16567

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