NLRP3-IN-83
NLRP3-IN-83 is a selective and orally active NLRP3 inflammasome activation inhibitor. NLRP3-IN-83 exhibits good inhibitory IL-1β activity with an IC50 of 1.4 μM by blocking NLRP3, independent of NF-κB signaling. NLRP3-IN-83 only slightly inhibits AIM2 inflammasome pathway, but has no effect on NLRC4 inflammasome. NLRP3-IN-83 prevent cell pyroptosis and exhibits significant anti-inflammatory efficacy in ulcerative colitis model. NLRP3-IN-83 can be used for the study of inflammatory bowel disease (IBD).
For research use only. We do not sell to patients.
- Formula: C17H16N2O2
- Molecular Weight:280.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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NLRP3 inflammasome |
IL-1β 1.4 μM (IC50) |
NLRP3-IN-83 (Compound 10) (0.625-5 μM, 1-25 h) significantly inhibits IL-1β release in LPS (HY-D1056)-primed J774A.1, LPS -primed murine BMDMs with Nigericin (HY-127019) or SiO2, and a PMA (HY-18739)-differentiated human THP-1 macrophage model in a concentration-dependent manner[1].
NLRP3-IN-83 (1-5 μM, 2 h) significantly reduced the levels of caspase-1 (p20) and IL-1β in the supernatants, while not affecting the expression levels of pro-caspase-1, pro-IL-1β, NLRP3, and ASC in LPS-primed J774A.1 cells[1].
NLRP3-IN-83 (1-5 μM) can prevent cell pyroptosis by inhibiting the cleavage of GSDMD and reducing the release of LDH in LPS-primed J774A.1 cells[1].
NLRP3-IN-83 (2.5-10 μM, 24 h) shows no significant toxicity to J774A.1 macrophages and human embryonic kidney cells HEK-293T[1].
NLRP3-IN-83 (1-5 μM, 2-6 h) inhibits NLRP3 inflammasome activation and has no significant effect on the NF-κB signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-primed J774A.1 or BMDMs, THP-1 cells
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Concentration:0.625, 1.25 and 2.5 μM (J774A.1 cells); 1,2, and 5 μM (others)
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Incubation Time:1 h and stimulated with Nigericin for 1 h; with SiO2 for 8 h; with PMA for 24 h
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Result:Significantly inhibited the release of IL-1β, showing a clear concentration-dependent effect.
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Cell Line:LPS-primed J774A.1 cells
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Concentration:LPS-primed J774A.1 cells
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Incubation Time:1 h and stimulated with Nigericin for 1 h
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Result:Reduced the production of caspase-1 (p20) and decreased the level of mature IL-1β (p17).
Did not affect the expression levels of pro-caspase-1, pro-IL-1β, NLRP3 and ASC.
Inhibited the self-oligomerization process of NLRP3.
Reduced the binding of NLRP3 to the adaptor protein ASC.
Significantly inhibited the formation of ASC oligomers.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced ulcerative colitis model established in 6-8-week-old C57BL/6 mice[1]
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Dosage:10 and 20 mg/kg
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Administration:Intragastric administration (i.g.), once daily for 7 days
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Result:Significantly improved symptoms of weight loss and rectal bleeding and shortening.
Significantly alleviated the pathological changes in the tissue (such as mucosal ulcers, crypt loss, inflammatory infiltration, etc.).
Dose-dependently reduced IL-1β, down-regulated NLRP3 and caspase-1 expression.
Chemical Information
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Molecular Weight 280.32
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Formula C17H16N2O2
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SMILES
OC1=C2C(C=CC(CNC3=CC=C(OC)C=C3)=N2)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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