2. Immunology/Inflammation
  3. NOD-like Receptor (NLR)
  4. CY-09

CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.

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CAS 番号 : 1073612-91-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 93 在庫あり
Solution
10 mM * 1 mL in DMSO USD 93 在庫あり
Solid
1 mg $60 在庫あり
5 mg $85 在庫あり
10 mg $145 在庫あり
25 mg $300 在庫あり
50 mg $485 在庫あり
100 mg $780 在庫あり
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カスタマーレビュー

Based on 50 publication(s) in Google Scholar

Other Forms of CY-09:

CY-09 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
RT-PCR
ELISA
Flow Cytometry
IF

    CY-09 purchased from MedChemExpress. Usage Cited in: Cell Res. 2025 Apr 1.  [Abstract]

    CY-09 (20 μM; 30 min) blocked NLRP3 inflammasome activation in THP-1 cells.

    CY-09 purchased from MedChemExpress. Usage Cited in: Cell Res. 2025 Apr 1.  [Abstract]

    CY-09 (20 μM; 30 min) suppressed NLRP3 activation induced by 1,5-PD and 1,2-PD in THP-1 cells.

    CY-09 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2022 Dec;113(Pt B):109430.

    CY09 remarkably inhibits the infiltration of CD11b+ myeloid cells in colon tumors of C. tropicalis-gavaged CAC mice.

    CY-09 purchased from MedChemExpress. Usage Cited in: J Orthop Surg Res. 2022 Nov 16;17(1):487.  [Abstract]

    Daphnoretin or CY-09 markedly attenuates the expression of COX-2, iNOS, TNF-α, IL-6, PGE2 and the NLRP3-ASC-Caspase1 infammasome in ATDC5 cells.

    CY-09 purchased from MedChemExpress. Usage Cited in: Blood. 2020 Jul 23;136(4):501-515.  [Abstract]

    CY-09 (1 μM; 24 h) suppressed TMAO-induced mRNA expression of M1 signature cytokines or chemokines in BMDMs, including IL-1β, IL-6, TNF-α, CXCL9, and CXCL10.

    CY-09 purchased from MedChemExpress. Usage Cited in: Blood. 2020 Jul 23;136(4):501-515.  [Abstract]

    CY-09 (1 μM; 24 h) markedly decreased the concentrations of IL-1β in the supernatant of BMDMs.

    CY-09 purchased from MedChemExpress. Usage Cited in: Blood. 2020 Jul 23;136(4):501-515.  [Abstract]

    CY-09 (1 μM; 24 h). Flow cytometry analysis of FLICA Casapse-1 in BMDMs was determined.

    NOD-like Receptor (NLR) アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    NLRP3 NLRP1 NOD1 NOD2

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation[1].

    IC50 & Target

    NLRP3

     

    体外実験

    CY-09 exhibits a dose-dependent inhibitory effect on monosodium urate (MSU), nigericin, ATP-induced caspase-1 activation and IL-1β secretion at the doses of 1 to10 μM in LPS-primed bone marrow-derived macrophages (BMDMs). Cytosolic LPS-induced noncanonical NLRP3 activation in BMDMs can also be blocked by CY-09 treatment. CY-09 specifically inhibits NLRP3 inflammasome activation and has no effect on LPS-induced priming effects. CY-09 treatment remarkably suppresses nigericin-induced ASC oligomerization. It is found that CY-09 treatment inhibits the interaction of Flag-NLRP3 and mCherry-NLRP3 in HEK-293T cells, suggesting that CY-09 blocks NLRP3 oligomerization[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    CY-09 関連抗体
    体内実験

    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 NLRP3 mutant mice up to days 30 to 48 even after treatment is stopped at day 25. The caspase-1 cleavage observed in adipose tissue of high-fat diet (HFD)-treated mice is also suppressed by CY-09[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    423.43

    分子式

    C19H12F3NO3S2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC(C1=CC=C(/C=C2SC(N(CC3=CC=CC(C(F)(F)F)=C3)C\2=O)=S)C=C1)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 150 mg/mL (354.25 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3617 mL 11.8083 mL 23.6167 mL
    5 mM 0.4723 mL 2.3617 mL 4.7233 mL
    10 mM 0.2362 mL 1.1808 mL 2.3617 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    一般には略語で表示されます：C1V1 = C2V2

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 1.5 mg/mL (3.54 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
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    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション
    参考文献
    キナーゼ実験
    [1]

    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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3617 mL 11.8083 mL 23.6167 mL 59.0416 mL
    5 mM 0.4723 mL 2.3617 mL 4.7233 mL 11.8083 mL
    10 mM 0.2362 mL 1.1808 mL 2.3617 mL 5.9042 mL
    15 mM 0.1574 mL 0.7872 mL 1.5744 mL 3.9361 mL
    20 mM 0.1181 mL 0.5904 mL 1.1808 mL 2.9521 mL
    25 mM 0.0945 mL 0.4723 mL 0.9447 mL 2.3617 mL
    30 mM 0.0787 mL 0.3936 mL 0.7872 mL 1.9681 mL
    40 mM 0.0590 mL 0.2952 mL 0.5904 mL 1.4760 mL
    50 mM 0.0472 mL 0.2362 mL 0.4723 mL 1.1808 mL
    60 mM 0.0394 mL 0.1968 mL 0.3936 mL 0.9840 mL
    80 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7380 mL
    100 mM 0.0236 mL 0.1181 mL 0.2362 mL 0.5904 mL
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    CY-09 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    CY-091073612-91-5CY09CY 09NOD-like Receptor (NLR)Inhibitorinhibitorinhibit

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    製品名:
    CY-09
    製品番号:
    HY-103666
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