WedelolactoneInhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis

Wedelolactone (CAS 524-12-9)

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Synonym: 7-Methoxy-5,11,12-trihydroxycoumestan; IKK Inhibitor II; Eclipta alba
Application: Inhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis
CAS Number: 524-12-9
Purity: ≥98%
Molecular Weight: 314.25
Molecular Formula: C16H10O7
* Refer to Certificate of Analysis for lot specific data (including water content).
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Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies suggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies suggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin (sc-202763), and galactosamine, and inhibit 5-lipoxygenase (5-LO)) activity in porcine leukocytes.


References

1. Wong, S.M., et al. 1988. Arzneimittelforschung. 38: 661-665. PMID: 2458108
2. Melo, P.A. and Ownby, C.L. 1999. Toxicon. 37: 199-215. PMID: 9920492
3. Syed, S.D., et al. 2003. Phytother Res. 17: 420-421. PMID: 12722155
4. Kobori, M., et al. 2004. Cell Death Differ. 11: 123-130. PMID: 14526390

Usage :
Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/mL), and MeOH.
Storage :
Store at -20° C
Boiling Point :
~498.41° C at 760 mmHg (Predicted)
Density :
~1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.75
IC50 :
LPS-induced caspase-11 : IC50 = 35 µM ( LPS-treated BALB 3T3 cells); IKKα kinase : IC50 = <10 µM; IKKβ kinase : IC50 = <10 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5281813
MDL Number :
MFCD07778564
SMILES :
COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O

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Wedelolactone  Product Citations

See how others have used Wedelolactone. Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 30726742  Wang, B.|Lim, JH.|Kajikawa, T.|Li, X.|Vallance, BA.|Moutsopoulos, NM.|Chavakis, T.|Hajishengallis, G.| et al. 2019. Cell Rep. 26: 1614-1626.e5.

PMID: # 29864955  2018. Biomed. Pharmacother. 103: 1658-1663.

PMID: # 28009352  Lv, S. et al. 2017. Cell Death Differ. 24: 492-499.

PMID: # 25712931  Gabrielli, E. et al. 2015. Infect. Immun. 83: 1940-8.

PMID: # 25631491  Huang, W. et al. 2015. Toxicol. Sci. 145: 68-79.

PMID: # 26381186  Upchurch, KC. et al. 2015. Immunol. Lett. 168: 89-97.

Citations 1 to 6 of 6 total
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