Avistron Chemistry Services ::: Product Detail ::: MCC950

MCC950 is a potent, selective and orally available inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

MCC950 (also known as CRID3 and CP-456,773)has demonstrated in vivo activity in multiple NLRP3-dependent mouse models1 and in ex vivo samples from individuals with CAPS. MCC950 is thus a potential therapeutic for NLRP3-associated syndromes, including autoinflammatory and autoimmune diseases, and a valuable tool for study of the NLRP3 inflammasome in human health and disease.

MCC950 is always available from stock, as the Sodium salt CAS: 256373-96-3 for immediate dispatch from Avistron Chemistry Services in a number of pack sizes, 5mg, 10mg, 25mg, 50mg,100mg.

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• MCC950 has an IC50 of 7.5 nM in BMDMs, Oral bioavailability = 68% & Half-Life = 3.27hr
• Demonstrates specific Inhibition of IL-1β secretion , leaving LPS-dependent TNF-α secretion unimpaired
• Shows no inhibition of NLRC4, AIM2, NLRP3 priming or Toll-like receptor signalling

The NLR family protein NLRP3 is an intracellular signaling molecule that senses many pathogen-derived, environmental and host-derived factors2. Upon activation, NLRP3 binds to apoptosis-associated speck-like protein containing a CARD (ASC). ASC in turn interacts with the cysteine protease caspase-1 to form a complex termed the inflam¬masome. This results in the activation of caspase-1, which cleaves the proinflammatory cytokines IL-1β and IL-18 to their active forms and mediates a type of inflammatory cell death known as pyroptosis3. Other intracellular pattern recognition receptors (PRRs) are also capable of forming inflammasomes. These include other NLR family members such as NLRP1 and NLRC4, as well as non-NLR PRRs such as the double-stranded DNA (dsDNA) sensors absent in melanoma 2 (AIM2) and interferon, gamma inducible protein 16 (IFI16)4. NLRP3-dependent IL-1β processing can also be activated by an indirect, non¬canonical pathway downstream of caspase-115

1. Coll, R.C., Robertson, A.A.B., Chae, J.J., Higgins, S.C., Muñoz-Planillo, R., Inserra, M.C., Vetter, I., Dungan, L.S., Monks, B.G., Stutz, A., Croker, D.E., Butler, M.S., Haneklaus, M., Sutton, C.E., Núñez, G., Latz, E., Kastner, D.L., Mills, K.H.G., Masters, S.L., Schroder, K., Cooper, M.A., O’Neill, L.A.J. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature Medicine, 21,248–255 (2015)
2. Wen, H., Miao, E.A. & Ting, J.P. Mechanisms of NOD-like receptor-associated inflammasome activation. Immunity 39, 432–441 (2013).
3. Schroder, K. & Tschopp, J. The inflammasomes. Cell 140, 821–832 (2010).
4. Latz, E., Xiao, T.S. & Stutz, A. Activation and regulation of the inflammasomes. Nat. Rev. Immunol. 13, 397–411 (2013).
5. Lamkanfi, M. & Dixit, V.M. Mechanisms and functions of inflammasomes. Cell 157, 1013–1022 (2014).

A number of other key references are given below:-

Nature Reviews Immunology 15, 199 (2015)

Nature Reviews Neurology 11, 186 (2015)

Nature Reviews Drug Discovery 14, 237 (2015)

Cell Metabolism Volume 21, Issue 4, p513–514, 2015

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