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CY-09

Catalog No. T4164 CAS 1073612-91-5

Synonyms: CY 09

CY-09 is an NLRP3 inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

CY-09, CAS 1073612-91-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 47.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 118.00
25 mg	In stock	$ 247.00
50 mg	In stock	$ 392.00
100 mg	In stock	$ 589.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 100%

Biological Description

Chemical Properties

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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].

Synonyms	CY 09
Molecular Weight	423.43
Formula	C19H12F3NO3S2
CAS No.	1073612-91-5

Storage

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

Solubility Information

DMSO: 77 mg/mL(181.8 mM)

References and Literature

1. Jiang H, et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov 6;214(11):3219-3238. 2. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway[J]. Redox Biology. 2020: 101534. 3. Chen Z, Zhang S, Nie B, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway[J]. Redox Biology. 2020: 101534.

Citations

1. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway. Redox Biology. 2020: 101534. 2. Jia Y, Cui R, Wang C, et al. Metformin protects against intestinal ischemia-reperfusion injury and cell pyroptosis via TXNIP-NLRP3-GSDMD pathway. Redox Biology. 2020: 101534. 3. Zhang Y, Liu Y, Xie Z, et al.Inhibition of PFKFB Preserves Intestinal Barrier Function in Sepsis by Inhibiting NLRP3/GSDMD.Oxidative Medicine and Cellular Longevity.2022, 2022. 4. Zhu Q, Zheng F, You W, et al.Expression of histone H1 in rats with traumatic brain injury and the effect of the NLRP3 inflammasome pathway.World Neurosurgery.2022

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Antidepressant Compound Library HIF-1 Signaling Pathway Compound Library Nonsteroidal Anti-Inflammatory Compound Library Anti-Ovarian Cancer Compound Library Fluorochemical Library NF-κB Signaling Compound Library Covalent Inhibitor Library Anti-Liver Cancer Compound Library Anti-Diabetic Compound Library

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Keywords

CY-09 1073612-91-5 Immunology/Inflammation NF-Κb NOD NOD-like Receptor (NLR) CY09 Inhibitor inhibit CY 09 inhibitor

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