2. Immunology/Inflammation
  3. NOD-like Receptor (NLR) Interleukin Related
  4. NLRP3-IN-39

NLRP3-IN-39 (Compound 49) inhibits the assembly and activation of NLRP3 inflammatory vesicles. NLRP3-IN-39 exerts its inhibitory effect by covalently binding to Cys 279 of the NLRP3 protein. NLRP3-IN-39 inhibits Nigericin (HY-127019)-induced IL-1β release from THP-1 cells (IC50= 0.29 μM).

For research use only. We do not sell to patients.

NLRP3-IN-39 Chemical Structure

NLRP3-IN-39 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

NLRP3-IN-39 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NLRP3-IN-39 (Compound 49) inhibits the assembly and activation of NLRP3 inflammatory vesicles. NLRP3-IN-39 exerts its inhibitory effect by covalently binding to Cys 279 of the NLRP3 protein. NLRP3-IN-39 inhibits Nigericin (HY-127019)-induced IL-1β release from THP-1 cells (IC50= 0.29 μM)[1].

IC50 & Target

NLRP3

 

IL-1β

 

In Vitro

NLRP3-IN-39 can inhibit Nigericin-induced IL-1β release in various cell types, with IC50 values of 0.29 μM in THP-1 cells, 44.97 nM in PBMCs, and 738.8 nM in BMDMs,respectively[1].
NLRP3-IN-39 (0-1 μM; 24 h) effectively inhibits the secretion of inflammatory cytokines in THP-1 cells and BMDMs without affecting the expression of precursor proteins[1].
NLRP3-IN-39 (0-1 μM; 40 min) significantly inhibits LDH release and pyroptosis induced by NLRP3 inflammasome activation in THP-1 cells and BMDMs. In LPS-primed THP-1 cells, NLRP3-IN-3 shows a significant, concentration-dependent inhibition of nigericin-induced IL-1β release[1].
NLRP3-IN-39 (0-1 μM; 40 min) significantly inhibits LDH release and pyroptosis induced by NLRP3 inflammasome activation in THP-1 cells and BMDMs. In LPS-primed THP-1 cells, NLRP3-IN-39 shows a significant, concentration-dependent inhibition of Nigericin-induced IL-1β release[1].
NLRP3-IN-39 (1 μM; 24 h) reduces the formation of ASC oligomers and ASC specks in Nigericin-induced THP-1 cells, while this phenomenon is not observed in NLRP3 KO THP-1 cells[1].

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

NLRP3-IN-39 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 cells and BMDMs
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 24 h
Result: Inhibited the secretion of IL-1β and caspase-1 in a concentration-dependent manner in LPS/nigericin-induced THP-1 cells and BMDMs, without significantly affecting the expression of pro-IL-1β (p31), pro-caspase-1 (p45), NLRP3, and ASC.

Immunofluorescence[1]

Cell Line: THP-1 cells and BMDMs
Concentration: 0, 0.25, 0.5, 1 μM
Incubation Time: 40 min
Result: Inhibits the red fluorescence of pyroptosis in a concentration-dependent manner, showing effects similar to MCC950 (HY-12815).
In Vivo

NLRP3-IN-39 (15, 30 mg/kg; i.p.; single dose) exhibits significant anti-inflammatory effects in a DSS-induced ulcerative colitis mouse model[1].
NLRP3-IN-39 is prepared in 5% DMSO and 95% saline to a concentration of 3 mg/mL.


Pharmacokinetic Analysis in C57BL/6 male mice[1]


Route Dose (mg/kg) AUC0−t (ng·h/mL) MRT0−t (h) Tmax (h) T1/2 (h) Cmax (ng/mL) Clz/F (L/h/kg)
i.p. 30 16.75 ± 0.69 10.98 ± 0.56 0.78 ± 0.61 6.83 ± 1.17 1.57 ± 0.19 68.7 637.40 ± 136.40

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

Animal Model: DSS-induced ulcerative colitis mouse model [1]
Dosage: 15, 30 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced the increased thickness of colonic tissue, crypt loss, goblet cell depletion, severe mucosal damage, and severe ulcer formation.
Significantly lowered the levels of IL-1β and TNF-α in colonic tissue and inhibited the activation of caspase-1.
Molecular Weight

422.30

Formula

C21H21Cl2NO4
Unlabeled CAS

SMILES

C[C@]12[C@]([H])(C([C@@H](CC2)OC(C3=C(C=C(N=C3)Cl)Cl)=O)=C)C[C@]4([H])C(C(O[C@@]4(C1)[H])=O)=C
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NLRP3-IN-39 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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-39NOD-like Receptor (NLR)Interleukin RelatedILAnti-inflammatory compoundIL-1β inhibitorDSS-induced colitis,Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NLRP3-IN-39
Cat. No.:
HY-161579
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.