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INF39

Catalog No. T4217   CAS 866028-26-4

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

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INF39 Chemical Structure
INF39, CAS 866028-26-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 56.00
2 mg In stock $ 79.00
5 mg In stock $ 122.00
10 mg In stock $ 172.00
25 mg In stock $ 363.00
50 mg In stock $ 543.00
100 mg In stock $ 783.00
500 mg In stock $ 1,620.00
1 mL * 10 mM (in DMSO) In stock $ 143.00
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Purity: 99.78%
Purity: 99.67%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.
In vitro INF39 possibly reacts with Cys-SH residues in the active site of cysteine protease caspase-1 but does not directly inhibit caspase-1 activity. INF39 (10 μM) can markedly inhibit ATP- and nigericin-induced IL-1β release. In the macrophages, INF39 suppresses caspase-1 activation and pyroptosis. INF39 can also block the NF-κB pathway. INF39 can reduce the steady-state (or basal) BRET signal of NLRP3, and not affect the viability of cells. INF39 cannot affect the initial conformational changes suffered by NLRP3 upon sensing the decrease of intracellular K+, but it affects the second step of NLRP3 conformational change. INF39 reaches the intestinal epithelium without undergoing chemical modifications. It is likely to act locally at the mucosal epithelial level after absorption into epithelial cells.
In vivo INF39 (p.o.) reduces systemic and colonic inflammation in rats treated with 2,4- dinitrobenzene sulfonic acid. In inflamed rats, INF39 (12.5/25/50 mg/ kg) markedly increases body weight. DNBS causes a significant increment of spleen weight (+39.3%). This increase is markedly 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 can dose-dependently attenuate the decrease in colonic length (?19, ?13 and ?8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 shows 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).
Cell Research Human THP-1 cells were exposed to INF39 (0.1?100 μM, 72 h), and then cell viability was evaluated by the MTT assay.
Animal Research Animal Models: Male Sprague?Dawley rats. Solvent: olive oil. Dosages: 12.5,25.0,50.0 mg/kg/day,p.o.
Molecular Weight 224.68
Formula C12H13ClO2
CAS No. 866028-26-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (44.51 mM)

TargetMolReferences and Literature

1. Cocco M, et al. J Med Chem. 2017, 60(9):3656-3671.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Inhibitor Library HIF-1 Signaling Pathway Compound Library Antidepressant Compound Library Covalent Inhibitor Library Anti-Breast Cancer Compound Library Bioactive Compounds Library Max NF-κB Signaling Compound Library Anti-Liver Cancer Compound Library Anti-Ovarian Cancer Compound Library

Related Products

Related compounds with same targets
D359-0396 Trimethylamine N-oxide NLRP3 agonist 1 NLRP3-IN-23 CORM-3 Arglabin Stavudine INF200

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Keywords

INF39 866028-26-4 Immunology/Inflammation NF-Κb NOD NOD-like Receptor (NLR) inhibit INF 39 INF-39 Inhibitor inhibitor

 

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