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CY-09

CY-09
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CY-09

Catalog No. T4164Cas No. 1073612-91-5
CY-09 is an NLRP3 inhibitor.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePrice/USDAvailabilityQuantity
1 mg$47In Stock
5 mg$68In Stock
10 mg$118In Stock
25 mg$247In Stock
50 mg$392In Stock
100 mg$589In Stock
1 mL x 10 mM (in DMSO)$75In Stock
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Product Introduction

Bioactivity
Description
CY-09 is an NLRP3 inhibitor.
In vitro
CY-09 demonstrates a dose-dependent decrease in monosodium urate (MSU), nigericin, and ATP-triggered caspase-1 activity and IL-1β release across 1 to 10 μM concentrations in LPS-primed bone marrow-derived macrophages (BMDMs). It effectively prevents cytosolic LPS-induced noncanonical NLRP3 activation in BMDMs. Notably, CY-09, like MCC950, selectively curbs NLRP3 inflammasome activity without impacting LPS-induced priming effects. Additionally, CY-09 significantly hinders nigericin-induced ASC oligomerization and disrupts Flag-NLRP3 and mCherry-NLRP3 interactions in HEK-293T cells, indicating a blockage of NLRP3 oligomerization by CY-09.
In vivo
Compare with MCC950, CY-09 treatment?in vivo?efficiently suppresses monosodium urate (MSU) injection-induced IL-1β production and neutrophil influx, suggesting that CY-09 can block MSU-induced NLRP3 inflammasome activation?in vivo. CY-09 treatment also increases the survival of?NLRP3mutant mice up to days 30 to 48 even after treatment is stopped at day 25. The caspase-1 cleavage observed in adipose tissue of HFD-treated mice is also suppressed by CY-09
Kinase Assay
For ATPase activity assay, purified recombinant human proteins are incubated at 37°C with indicated concentrations of CY-09 for 15 min in the reaction buffer. ATP (25 μM) is then added, and the mixture is further incubated at 37°C for another 40 min. The amount of ATP converted into adenosine diphosphate (ADP) is determined by luminescent ADP detection with ADP-Glo Kinase Assay kit according to the manufacturer's protocol. The results are expressed as percentage of residual enzyme activity to the vehicle-treated enzyme. For ATP binding assay, purified NLRP3 proteins are incubated with ATP binding agarose for 1 h and then different concentrations of CY-09 are added and incubated for 2 h with motion at 4°C. Beads are washed and boiled in loading buffer. Samples are subjected to immunoblotting analysis[1].
Cell Research
To induce NLRP3 inflammasome activation, 5×105/mL BMDMs and 6×106/mL PBMCs are plated in 12-well plates. The following morning, the medium is replaced, and cells are stimulated with 50 ng/mL LPS or 400 ng/mL Pam3CSK4 (for noncanonical inflammasome activation) for 3 h. After that, CY-09 or other inhibitors are added into the culture for another 30 min, and then the cells are stimulated for 4 h with monosodium urate (MSU) (150 μg/mL),?Salmonella typhimurium?(multiplicity of infection) or for 30 min with ATP (2.5 mM) or nigericin (10 μM). Cells are transfected with poly(dA:dT) (0.5 μg/mL) for 4 h or LPS (500 ng/mL) overnight. Cell extracts and precipitated supernatants are analyzed by immunoblot[1].
Animal Research
For the?in vivo?experiments, CY-09 is formulated in a vehicle containing 10% DMSO, 10% Solutol HS 15, and 80% saline,WT or Nlrp3?/? mice at the age of 6 wk, with similar plasma glucose levels and body weights are randomized into different groups. For generation of high-fat diet (HFD)-induced diabetic mice, mice are fed with HFD for 14 wk. The diabetic mice are treated with CY-09 (i.p.) at a dose of 2.5 mg/kg once a day for 6 wk. The mice are maintained with HFD when used for CY-09 treatment and the subsequent experiments[1].
AliasCY 09
Chemical Properties
Molecular Weight423.43
FormulaC19H12F3NO3S2
Cas No.1073612-91-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 77 mg/mL(181.8 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3617 mL11.8083 mL23.6167 mL118.0833 mL
5 mM0.4723 mL2.3617 mL4.7233 mL23.6167 mL
10 mM0.2362 mL1.1808 mL2.3617 mL11.8083 mL
20 mM0.1181 mL0.5904 mL1.1808 mL5.9042 mL
50 mM0.0472 mL0.2362 mL0.4723 mL2.3617 mL
100 mM0.0236 mL0.1181 mL0.2362 mL1.1808 mL

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