1. Immunology/Inflammation Apoptosis
  2. NOD-like Receptor (NLR) AIM2 Pyroptosis
  3. NLRP3/AIM2-IN-3

NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization.

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NLRP3/AIM2-IN-3 Chemical Structure

NLRP3/AIM2-IN-3 Chemical Structure

CAS No. : 1787787-60-3

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Based on 4 publication(s) in Google Scholar

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Description

NLRP3/AIM2-IN-3 (compound 59) is a potent inhibitor with differential species specific effects against NLRP3 and AIM2 inflammasome-dependent pyroptosis. NLRP3/AIM2-IN-3 shows inhibitory efficacy against pyroptosis in THP-1 macrophages stimulated with LPS/nigericin, with an IC50 of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disturbs the interaction of NLRP3 or AIM2 with the adaptor protein ASC and inhibited ASC oligomerization[1].

IC50 & Target

NLRP3

 

In Vitro

NLRP3/AIM2-IN-3 (0-100 μM) displays remarkable inhibitory activity against NLRP3-and AIM2-but not NLRC4-dependent activation of caspase-1 and the release of IL-1b in human THP-1 macrophages[1].
NLRP3/AIM2-IN-3 shows inhibition of IL-1b secretion by human THP-1 macrophages, with IC50 of 0.098 μM, which is nearly 150-fold and 500-fold more potent than that of J774A.1 (14.62 μM) and bone marrow-derived macrophages (BMDMs) (48.98 μM), respectively[1].
NLRP3/AIM2-IN-3 has almost no inhibitory effect on the AIM2 inflammasome-dependent activation of caspase-1 and release of IL-1b in J774A.1 cells[1].

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

Molecular Weight

266.29

Formula

C16H14N2O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC=CC(O)=C1)CC2=CC3=C(C=C2)C=CN3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (938.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 50 mg/mL (187.77 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7553 mL 18.7765 mL 37.5530 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Methanol / DMSO 1 mM 3.7553 mL 18.7765 mL 37.5530 mL 93.8826 mL
5 mM 0.7511 mL 3.7553 mL 7.5106 mL 18.7765 mL
10 mM 0.3755 mL 1.8777 mL 3.7553 mL 9.3883 mL
15 mM 0.2504 mL 1.2518 mL 2.5035 mL 6.2588 mL
20 mM 0.1878 mL 0.9388 mL 1.8777 mL 4.6941 mL
25 mM 0.1502 mL 0.7511 mL 1.5021 mL 3.7553 mL
30 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1294 mL
40 mM 0.0939 mL 0.4694 mL 0.9388 mL 2.3471 mL
50 mM 0.0751 mL 0.3755 mL 0.7511 mL 1.8777 mL
60 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
80 mM 0.0469 mL 0.2347 mL 0.4694 mL 1.1735 mL
100 mM 0.0376 mL 0.1878 mL 0.3755 mL 0.9388 mL
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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.

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Product Name:
NLRP3/AIM2-IN-3
Cat. No.:
HY-144226
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