2. Immunology/Inflammation Apoptosis
  3. NOD-like Receptor (NLR) Pyroptosis Interleukin Related
  4. 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).

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NLRP3-IN-83

NLRP3-IN-83 Chemical Structure

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NLRP3-IN-83 Related Antibodies

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Description

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)[1].

IC50 & Target[1]

NLRP3 inflammasome

 

IL-1β

1.4 μM (IC50)

In Vitro

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.

NLRP3-IN-83 Related Antibodies

ELISA Assay[1]

Cell Line: LPS-primed J774A.1 or BMDMs, THP-1 cells
Concentration: 0.625, 1.25 and 2.5 μM (J774A.1 cells); 1,2, and 5 μM (others)
Incubation Time: 1 h and stimulated with Nigericin for 1 h; with SiO2 for 8 h; with PMA for 24 h
Result: Significantly inhibited the release of IL-1β, showing a clear concentration-dependent effect.

Western Blot Analysis[1]

Cell Line: LPS-primed J774A.1 cells
Concentration: LPS-primed J774A.1 cells
Incubation Time: 1 h and stimulated with Nigericin for 1 h
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.
In Vivo

NLRP3-IN-83 (Compound 10) (10-20 mg/kg, i.g., once daily for 7 days) exhibits significant anti-inflammatory efficacy in a DSS (HY-116282C)-induced ulcerative colitis model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: DSS-induced ulcerative colitis model established in 6-8-week-old C57BL/6 mice[1]
Dosage: 10 and 20 mg/kg
Administration: Intragastric administration (i.g.), once daily for 7 days
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.
Molecular Weight

280.32

Formula

C17H16N2O2
SMILES

OC1=C2C(C=CC(CNC3=CC=C(OC)C=C3)=N2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NLRP3-IN-83 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NLRP3-IN-83NOD-like Receptor (NLR)PyroptosisInterleukin RelatedILHydroxyquinolineInflammasomeIL-1βInflammatory bowel diseaseInhibitorinhibitorinhibit

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