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Caspase-1 and inflammasome inhibitor – Parthenolide

Parthenolide Unit size Cat. code Docs Qty Price
Caspase-1 and inflammasome inhibitor
50 mg
inh-ptd
+-
$174.00

Caspase-1 and inflammasome inhibitor

Parthenolide is a broad-spectrum inhibitor with numerous anti-inflammatory properties [1]. Its targets include NF‑κB, caspase-1, and multiple inflammasomes [1, 2].

INFLAMMASOMES:

The inflammasomes are innate immune sensors that drive the activation of inflammatory caspases including caspase-1. They are activated by a two-step process; a first signal (‘priming’) provided mainly by bacterial components or endogenous cytokines involves NF-κB induction, while the second signal provided by a wide array of stimuli including microbial toxins, endogenous molecules, or crystalline substances and leads to inflammasome assembly and activation. Numerous inflammasomes have been described among them the NLRP3 inflammasome has been best characterized [3].

MODE OF ACTION OF PARTHENOLIDE:

Parthenolide blocks the activity of the NLRP1, NLRP3, NLRC4 inflammasomes, but not the AIM2 inflammasome [2, 4, 5]. Mechanistically, it has been reported that parthenolide inhibits the IκB kinase function required for NF-κB activation [6], and alkylates the cysteine residues in caspase-1 and in the ATPase domain of NLRP3, thereby blocking their activity [1, 2].

KEY FEATURES OF PARTHENOLIDE:

  • Caspase-1 and NF-κB inhibitor
  • Inhibits the NLRP1, NLRP3, and NLRC4 inflammasomes
  • Each lot is highly pure (≥95%) and functionally tested

 

Read our review on inflammasomes.

 

 

References:

1. Zahid A. et al., 2019. Pharmacological Inhibitors of the NLRP3 Inflammasome. Front Immunol. 2019. 10(2538).
2. Juliana C. et al., 2010. Anti-inflammatory compounds parthenolide and Bay 11-7082 are direct inhibitors of the inflammasome. J Biol Chem. 285(13):9792-802.
3. Zheng, D. et al., 2020. Inflammasome activation and regulation: toward a better understanding of complex mechanisms. Cell Discov 6, 36.
4. Coll R.C. & O’Neill L.A.J., 2011. The cytokine release inhibitory drug CRID3 targets ASC oligomerisation in the NLRP3 and AIM2 inflammasomes. PLoS One. 6(12): e29539.
5. Honda H. et al., 2014. Isoliquiritigenin is a potent inhibitor of NLRP3 inflammasome activation and diet-induced adipose tissue inflammation. J Leukoc Biol. 96(6): 1087-100.
6. Saadane A. et al., 2007. Parthenolide inhibits IκB kinase, NF-κB activation, and inflammatory response in cystic fibrosis cells and mice. Am J Respir Cell Mol Biol. 36(6):728-36.
 

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Specifications

Solubility: 50 mg/ml (202 mM) in DMSO or ethanol

CAS number: 20554-84-1

Formula: C15H20O3

Molecular weight: 248 g/mol

Quality control:

  • Purity ≥95% (UHPLC)
  • The inhibitory activity of the product has been validated using the inflammasome inhibition assay.
  • The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
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Contents

  • 50 mg Parthenolide (provided as a powder)

Parthenolide 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 Parthenolide: 

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