1. Immunology/Inflammation
  2. NOD-like Receptor (NLR)
  3. INF39

INF39 

Cat. No.: HY-101868 Purity: 99.61%
Handling Instructions

INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.

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

INF39 Chemical Structure

INF39 Chemical Structure

CAS No. : 866028-26-4

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5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
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25 mg USD 440 In-stock
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50 mg USD 740 In-stock
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100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.

In Vitro

INF39 is able to significantly inhibit ATP- and nigericin-induced IL-1β release at 10 μM. INF39 reduces caspase-1 activation and pyroptosis in the macrophages. INF39 can block not only NLRP3 activation but also the NF-κB pathway. INF39 potentially reacts with Cys-SH residues in the active site of cysteine protease caspase-1, but does not directly target caspase-1 activity. INF39 is able to reduce the steady state (or basal) BRET signal of NLRP3 without affecting the viability of cells, meaning that it can interfere with the basal NLRP3 conformation. INF39 does not block the initial conformational changes suffered by NLRP3 upon sensing the decrease of intracellular K+; however, it affects a second step of NLRP3 conformational change that could be related with the ATPase activity of the receptor and be independent of the decrease of intracellular K+. INF39 reaches the intestinal epithelium without undergoing chemical modifications. After absorption into epithelial cells, it is likely to act locally at the mucosal epithelial level[1].

In Vivo

Oral administration of INF39 reduces systemic and colonic inflammation in rats treated with 2,4- dinitrobenzenesulfonic acid. Significant increments of body weight are observed in inflamed rats under treatment with INF39 (12.5, 25, and 50 mg/ kg). Treatment with DNBS results in a significant increment of spleen weight (+39.3%). Such an increase is significantly reduced by administration of INF39 (+2.2, +4.3 and +4.8% at 12.5, 25, 50 mg/kg, respectively). The inhibition of NLRP3 inflammasome complex with INF39 dose-dependently attenuates the decrease in colonic length (−19, −13 and −8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 displays a significant reduction of macroscopic damage score (4.7 at 12.5 mg/kg, 3.1 at 25 mg/kg, and 2.8 at 50 mg/kg). Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats[1].

Molecular Weight

224.68

Formula

C₁₂H₁₃ClO₂

CAS No.

866028-26-4

SMILES

O=C(OCC)C(CC1=CC=CC=C1Cl)=C

Shipping

Room temperature in continental US; may vary elsewhere

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

DMSO : 1 mg/mL (4.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4508 mL 22.2539 mL 44.5077 mL
5 mM --- --- ---
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

INF39 (100 μM final concentration, 2% DMSO) is added to wells containing immobilized NALP3 protein and preincubated for 55 min at 37°C to mimic normal experimental time (15 min preincubation+40 min incubation with ATP); in the control wells a mixture of buffer and DMSO is added. After the preincubation time the wells areished three times with reaction buffer, and ATP (250 μM) is added for 40 min at 37°C. ADP formation is measured with ADP-Glo-Assay[1].

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

Animal Administration
[1]

Rats:
DNBS-untreated and DNBS treated animals are assigned to the following treatment groups: INF39 (12.5, 25, 50 mg/kg/day) or dexamethasone (DEX, 1 mg/kg/day). INF39 and dexamethasone are suspended in olive oil and 1% methylcellulose, respectively, and administered in a volume of 0.2 mL/rat. DNBS-untreated animals (control group) and DNBS-treated rats (colitis group) received drug vehicle to serve as controls. Body weight is monitored daily starting from the onset of drug treatments[1].

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

References
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INF39
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