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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, CAS 866028-26-4

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Purity: 98%

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 2 years

Solubility Information

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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：

HIF-1 Signaling Pathway Compound Library Inhibitor Library Immunology/Inflammation Compound Library Covalent Inhibitor Library NF-κB Signaling Compound Library Nonsteroidal Anti-Inflammatory Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

Related Products

Related compounds with same targets

Emlenoflast Asymmetric dimethylarginine 6-Biopterin NLRP3-IN-10 L-Canavanine sulfate CY-09 MCC950 Imperatorin

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

INF39 866028-26-4 NF-Kb信号通路免疫与炎症 NOD NOD-like Receptor (NLR) inhibit INF 39 INF-39 Inhibitor inhibitor

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