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Immunology / Inflammation NOD INF39

INF39

Catalog No. T4217   CAS 866028-26-4
Purity 99.78% Datasheet

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

INF39, CAS 866028-26-4
Pack Size Availability Price/USD Quantity
1 mg In stock 83.00
2 mg In stock 105.00
5 mg In stock 150.00
10 mg In stock 210.00
25 mg In stock 440.00
1 mL * 10 mM (in DMSO) In stock 150.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.
Targets&IC50 NLRP3,  
Animal Research
Animal Models: Male Sprague−Dawley rats Solvent: olive oil Dosages: 12.5, 25.0, 50.0 mg/kg/day, p.o.
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.

Description

INF39 is a noncytotoxic and irreversible NLRP3 inhibitor.

Targets&IC50

NLRP3

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).

Animal Research

Animal Models: Male Sprague−Dawley rats Solvent: olive oil Dosages: 12.5, 25.0, 50.0 mg/kg/day, p.o.

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.

Synonyms
Purity 99.78%
Appearance solid
Molecular Weight 224.68
Formula C12H13ClO2
CAS No. 866028-26-4

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 10 mM

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

Citations

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:
Bioactive Compound Library Immunology/Inflammation Compound Library NF-κB Signaling Compound Library

Related Products

Related compounds with same targets
NLRP3 Inflammasome Inhibitor I Imperatorin NOD-IN-1 INF39 MCC950 Dapansutrile 4',7-Dihydroxyflavone CY-09

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.