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NLRP3 inflammasome inhibitor - MCC950

MCC950 Unit size Cat. code Docs Qty Price
NLRP3 inflammasome inhibitor
10 mg
inh-mcc
+-
$132.00

NLRP3 inflammasome inhibitor

Inhibition of the NLRP3 inflammasome by MCC950
Inhibition of the NLRP3 inflammasome by MCC950

MCC950 is potent and specific of the NLRP3  inflammasome [1,2].

The NLRP3 inflammasome is an innate immune sensor that is activated by a two-step process; a first signal (‘priming’) is provided by microbial molecules such as lipopolysaccharide (LPS), while the second signal is provided by a wide array of stimuli including microbial toxins, endogenous molecules or crystalline substances. This triggers inflammasome multimerization and caspase-1 activation with the subsequent maturation and secretion of interleukin-1β (IL-1β) and IL-18.

MCC950 blocks the release of IL‑1β induced by NLRP3 activators, such as nigericin, ATP, and MSU crystals [3,4]. It inhibits the NLRP3 inflammasome by directly targeting the NLRP3 NATCH domain and interfering with the Walker B motif function thus preventing NLRP3 conformational change and oligomerization [1,2]. In research models of inflammation, such as cryopyrin-associated periodic syndromes (CAPS) and myocardial infarction, MCC950 effectively inhibited NLRP3-induced IL-1β production [3-5]. Importantly, MCC950 does not inhibit the AIM2, NLRC4, or NLRP1 inflammasomes [4].

 

Key features of MCC950:

  • Potent and specific inhibitor of the NLRP3 inflammasome
  • Does not inhibit the AIM2, NLRC4 or NLRP1 inflammasomes
  • Each lot is highly pure (≥98%) and functionally tested

 

Read our review on the NLRP3 inflammasome.

 

References:

1. Tapia-Abellán A. et al., 2019. MCC950 closes the active conformation of NLRP3 to an inactive state. Nature Chemical Biology. 15(6):560-4.
2. Coll R.C. et al., 2019. MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition. Nature Chemical Biology. 15(6):556-9.
3. Guo H. et al., 2015. Inflammasomes: mechanism of action, role in disease, and therapeutics. Nat Med. 21(7):677-87.
4. Coll RC. et al., 2015. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature Med 21(3), 248-255.
5. van Hout GP. et al., 2016. The selective NLRP3-inflammasome inhibitor MCC950 reduces infarct size and preserves cardiac function in a pig model of myocardial infarction. Eur Heart J. ehw247.

 

 

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Specifications

CAS number: 210826-40-7

Working concentration: 300 nM (121.34 ng/ml) to 10 μM (4.04 μg/ml) for cell culture assays

Solubility: DMSO (10 mg/ml)

Formula: C20H24N2O5S

Molecular weight: 404.48 g/mol

Quality control:

  • Purity: ≥98% (UHPLC)
  • The inhibitory activity of the product has been validated using cellular assays.
  • The absence of bacterial contamination (e.g. lipoproteins and endotoxins) is confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
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Contents

  • 10 mg MCC950 (provided as a translucent film)

MCC950 is shipped at room temperature.

Store at -20 °C.

Resuspended product is stable for at least 6 months when properly stored.

Alert Avoid repeated freeze-thaw cycles.

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Details

Chemical structure of MCC950: 

MCC950 chemical structure

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