CY-09

Catalog No.S5774 Batch:S577401

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Technical Data

Formula

C19H12F3NO3S2

Molecular Weight 423.43 CAS No. 1073612-91-5
Solubility (25°C)* In vitro DMSO 85 mg/mL (200.74 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description CY-09 is a specific NLRP3 inflammasome inhibitor that directly targeted NLRP3 itself. It is tested against the five major cytochrome P450 enzymes 1A2, 2C9, 2C19, 2D6, and 3A4 with half maximal inhibitory concentration (IC50) values of 18.9, 8.18, >50, >50, and 26.0 µM, respectively.
Targets
NLRP3 inflammasome [1]
In vitro

CY-09 specifically blocks NLRP3 activation in macrophages. CY-09 inhibits NLRP3 oligomerization and inflammasome assembly. CY-09 directly binds to NLRP3 and inhibits its ATPase activity. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes. The metabolic stability of CY-09 was first evaluated using human and mouse liver microsomes, exhibiting favorable stability with the half-life >145 min for both human and mouse microsomes, which exhibited low risk of drug-drug interactions[1].

In vivo

CY-09 inhibits NLRP3 activation in vivo and prevents neonatal lethality in a mouse model of CAPS. In pharmacokinetic studies evaluted in C57BL/6J mice administered a single i.v. or oral dose, CY-09 exhibits favorable pharmacokinetics, with a half-life of 2.4 h, an area under the curve of 8,232 (h·ng)/ml, and bioavailability of 72%. CY-09 reverses metabolic disorders in diabetic mice by inhibition of NLRP3-dependent inflammation. CY-09 treatment has remarkable beneficial effects for metainflammation, hyperglycemia, and insulin resistance in diabetic mice[1].

Protocol (from reference)

Cell Assay:

[1]

  • Cell lines

    BMDMs and PBMCs

  • Concentrations

    1, 5, and 10 μM

  • Incubation Time

    30 min

  • Method

    5 × 105/ml BMDMs and 6 × 106/ml PBMCs were plated in 12-well plates. The following morning, the medium was replaced, and cells were 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 were added into the culture for another 30 min, and then the cells were stimulated for 4 h with MSU (150 µg/ml), Salmonella typhimurium (multiplicity of infection) or for 30 min with ATP (2.5 mM) or nigericin (10 µM). Cells were transfected with poly(dA:dT) (0.5 µg/ml) for 4 h or LPS (500 ng/ml) overnight. Cell extracts and precipitated supernatants were analyzed by immunoblot.

Animal Study:

[1]

  • Animal Models

    C57BL/6J mice

  • Dosages

    5 and 10 mg/kg

  • Administration

    i.v. and oral administration

Selleck's CY-09 has been cited by 11 publications

FXR controls duodenogastric reflux-induced gastric inflammation through negatively regulating ER stress-associated TNXIP/NLPR3 inflammasome [ iScience, 2024, 27(3):109118] PubMed: 38439955
Inhibiting NLRP3 Inflammasome Activation by CY-09 Helps to Restore Cerebral Glucose Metabolism in 3×Tg-AD Mice [ Antioxidants (Basel), 2023, 12(3)722] PubMed: 36978970
Autophagy-based unconventional secretion of HMGB1 in glioblastoma promotes chemosensitivity to temozolomide through macrophage M1-like polarization [ J Exp Clin Cancer Res, 2022, 41(1):74] PubMed: 35193644
PEG2-Induced Pyroptosis Regulates the Expression of HMGB1 and Promotes hEM15A Migration in Endometriosis [ Int J Mol Sci, 2022, 23(19)11707] PubMed: 36233009
MiR-624-5p enhances NLRP3 augmented gemcitabine resistance via EMT/IL-1β/Wnt/β-catenin signaling pathway in ovarian cancer [ J Reprod Immunol, 2022, 150:103488] PubMed: 35124344
CY-09 attenuates the progression of osteoarthritis via inhibiting NLRP3 inflammasome-mediated pyroptosis [ Biochem Biophys Res Commun, 2021, 553:119-125] PubMed: 33765556
Low-density lipoprotein receptor (LDLR) regulates NLRP3-mediated neuronal pyroptosis following cerebral ischemia/reperfusion injury [ J Neuroinflammation, 2020, 17(1):330] PubMed: 33153475
Activation of the Nlrp3 Inflammasome Contributes to Shiga Toxin-Induced Hemolytic Uremic Syndrome in a Mouse Model [ Front Immunol, 2020, 11:619096] PubMed: 33552083
TREM-1 Exacerbates Neuroinflammatory Injury via NLRP3 Inflammasome-Mediated Pyroptosis in Experimental Subarachnoid Hemorrhage [ Transl Stroke Res, 2020, 10.1007/s12975-020-00840-x] PubMed: 32862402
NLRP3 Augmented Resistance to Gemcitabine in Triple-Negative Breast Cancer cells(TNBCC) via EMT/IL-1β/Wnt/β-catenin Signaling Pathway [ Biosci Rep, 2020, BSR20200730] PubMed: 32578856

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.