CY-09 |
Catalog No.GC19113
One-Click Copy Product Info
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CY-09 is a selective NLRP3 inflammasome inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1073612-91-5
Sample solution is provided at 25 µL, 10mM.
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CY-09 is a selective NLRP3 inflammasome inhibitor. CY-09 directly binds to the ATP-binding motif of the NACHT domain of NLRP3 and inhibits NLRP3 ATPase activity, thereby blocking NLRP3 inflammasome assembly and activation. CY-09 can be used in research on NLRP3-driven diseases such as inflammatory diseases, type 2 diabetes, non-alcoholic fatty liver disease, post-myocardial infarction cardiac fibrosis, and Alzheimer's disease[1-4].
In vitro, THP-1 cells were pretreated with 20µM CY-09 for 30 minutes, then stimulated with 1µg/mL LPS for 3 hours and 4µM nigericin for 1 hour. CY-09 inhibited caspase-1 activation, mature IL-1β secretion, and LDH release[5]. Hyperglycemia-induced HK-2 cells were treated with 5-10µM CY-09 for 48 hours. CY-09 suppressed the elevated expression of NLRP3, caspase-1, IL-1β, and IL-18, reduced cleaved-caspase 3 levels, and downregulated fibronectin and α-smooth muscle actin expression[6]. 661W cells were co-treated with 25-100µM CY-09 and 500µg/mL NaIO3 for 24 hours. CY-09 increased 661W cell viability, decreased the apoptosis rate, and reduced the number of autophagosomes[7].
In vivo, C57BL/6J mice received a single intraperitoneal injection of 40mg/kg CY-09 30 minutes before an intraperitoneal injection of 1mg monosodium urate crystals. CY-09 inhibited monosodium urate-induced IL-1β production in serum and peritoneal lavage fluid and reduced Ly6G/CD11b-positive neutrophil recruitment[8]. C57BL/6J mice with transverse aortic constriction surgery were intraperitoneally injected with 2mg/kg CY-09 and ponatinib six times per week for 4 weeks. CY-09 preserved cardiac ejection fraction and fractional shortening, reduced splenic myeloid cell and neutrophil proliferation, and attenuated myocardial macrophage induction, T cell proliferation, and inflammatory monocyte expansion[9]. 3xTg-AD mice and NTg mice were intraperitoneally injected with 2.5mg/kg CY-09 for 6 consecutive weeks. CY-09 reduced cerebral NLRP3, pro-caspase-1, caspase-1, and IL-1β expression and IL-1β secretion, increased 18F-FDG standardized uptake values in the whole brain, cortex, and hippocampus and whole-brain glucose metabolic rate, lowered fasting and basal blood glucose and fasting insulin levels, and improved glucose tolerance and insulin sensitivity[10].
References:
[1] Yang Y, Wang H, Kouadir M, et al. Recent advances in the mechanisms of NLRP3 inflammasome activation and its inhibitors. Cell Death Dis. 2019 Feb 12;10(2):128.
[2] Zhang Y, Lin Z, Chen D, et al. CY-09 attenuates the progression of osteoarthritis via inhibiting NLRP3 inflammasome-mediated pyroptosis. Biochem Biophys Res Commun. 2021 May 14;553:119-125.
[3] Zheng Q, Yao D, Cai Y, et al. NLRP3 augmented resistance to gemcitabine in triple-negative breast cancer cells via EMT/IL-1β/Wnt/β-catenin signaling pathway. Bioscience Reports. 2020;40(8):BSR20200730.
[4] Sun K, Wang J, Lan Z, et al. Sleeve Gastroplasty Combined with the NLRP3 Inflammasome Inhibitor CY-09 Reduces Body Weight, Improves Insulin Resistance and Alleviates Hepatic Steatosis in Mouse Model. Obesity Surgery. 2020 Sep;30(9):3435-43.
[5] Zou G, Tang Y, Yang J, et al. Signal-induced NLRP3 phase separation initiates inflammasome activation. Cell Research. 2025;35(5):437-452.
[6] Yang M, Zhao L. The selective NLRP3-inflammasome inhibitor CY-09 ameliorates kidney injury in diabetic nephropathy by inhibiting NLRP3-inflammasome activation. Current Medicinal Chemistry. 2023;30(28):3261-70.
[7] Jiang H, He H, Chen Y, et al. Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders. J Exp Med. 2017 Nov;214(11):3219-38.
[8] Wang XL, Gao YX, Yuan QZ, et al. Protective effects of CY-09 and astaxanthin on NaIO3-induced photoreceptor inflammation via the NLRP3/autophagy pathway. Int J Ophthalmol. 2024 Jul 18;17(7):1217-31.
[9] Tousif S, Singh AP, Umbarkar P, et al. Ponatinib Drives Cardiotoxicity by S100A8/A9-NLRP3-IL-1β Mediated Inflammation. Circ Res. 2023 Feb 3;132(3):267-89.
[10] Han S, He Z, Hu X, et al. Inhibiting NLRP3 Inflammasome Activation by CY-09 Helps to Restore Cerebral Glucose Metabolism in 3xTg-AD Mice. Antioxidants. 2023 Mar 15;12(3):722.
| Cell experiment [1]: | |
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Cell lines |
HK-2 cells (human proximal tubular epithelial cell line) |
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Preparation Method |
HK-2 cells were maintained in DMEM/F12 medium supplemented with 10% FBS at 37°C, 5% CO2. HK-2 cells were treated with 5µM or 10µM CY-09 together with 30mM glucose for 48 hours; mRNA levels of NLRP3, caspase-1, IL-1β, IL-18 and fibrosis markers fibronectin and α-SMA were assessed by RT-PCR, cleaved-caspase 3 by Western blot. |
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Reaction Conditions |
5µM or 10µM; 48h |
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Applications |
CY-09 reduced high glucose-induced NLRP3, caspase-1, IL-1β and IL-18 mRNA expression, lowered cleaved-caspase 3 protein level, and decreased fibronectin and α-SMA expression in HK-2 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6J mice with transverse aortic constriction (TAC) |
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Preparation Method |
TAC-operated mice were intraperitoneally administered CY-09 (2mg/kg) six times per week together with ponatinib (15mg/kg/day by oral gavage) for 4 weeks; cardiac function was assessed by echocardiography, myocardial inflammatory cells and cytokine-producing cells by flow cytometry and immunostaining, and plasma cytokines by ELISA. |
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Dosage form |
2mg/kg; i.p.; 6 times/week for 4 weeks |
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Applications |
CY-09 nearly abolished ponatinib-induced decline in ejection fraction and fractional shortening, reduced frequencies of TNF-α-, IL-1β- and IL-6-producing cells in myocardium, decreased plasma TNF-α, IL-1β, IL-6 and S100A8/9 levels, and reduced proliferation of myeloid cells and neutrophils in spleen. |
References: [1] Yang M, Zhao L. The selective NLRP3-inflammasome inhibitor CY-09 ameliorates kidney injury in diabetic nephropathy by inhibiting NLRP3-inflammasome activation. Curr Med Chem. 2023;30(28):3261-70. [2] Tousif S, Singh AP, Umbarkar P, et al. Ponatinib Drives Cardiotoxicity by S100A8/A9-NLRP3-IL-1β Mediated Inflammation. Circ Res. 2023 Feb 3;132(3):267-89. | |
| Cas No. | 1073612-91-5 | SDF | |
| Canonical SMILES | OC(C1=CC=C(/C=C2SC(N(CC3=CC=CC(C(F)(F)F)=C3)C\2=O)=S)C=C1)=O | ||
| Formula | C19H12F3NO3S2 | M.Wt | 423.43 |
| Solubility | DMSO : ≥ 150 mg/mL (354.25 mM) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3617 mL | 11.8083 mL | 23.6167 mL |
| 5 mM | 472.3 μL | 2.3617 mL | 4.7233 mL |
| 10 mM | 236.2 μL | 1.1808 mL | 2.3617 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)