2. Immunology/Inflammation
  3. Cyclic GMP-AMP Synthase
  4. RU.521

RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).

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CAS 番号 : 2262452-06-0

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 132 在庫あり
Solution
10 mM * 1 mL in DMSO USD 132 在庫あり
Solid
1 mg $48 在庫あり
5 mg $120 在庫あり
10 mg $180 在庫あり
25 mg $335 在庫あり
50 mg $475 在庫あり
100 mg $700 在庫あり
500 mg $1750 在庫あり
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カスタマーレビュー

Based on 83 publication(s) in Google Scholar

RU.521 関連抗体

Top Publications Citing Use of Products

顧客検証

Bio/Physico-chemical Assay
RT-PCR
Histological Imaging/Staining
IF
WB

    RU.521 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 20;16(1):10222.  [Abstract]

    RU.521 (10 μM; 1 h). Ifnb1 expression (LPS 24 h) and interferon-β (IFN-β) release (LPS 6 h) in LPS-stimulated WT and m.5019 A > G macrophages pre-treated with cyclic GMP-AMP synthase (cGAS) inhibitor RU.521 for 1 h (n = 3).

    RU.521 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 3;16(1):289.  [Abstract]

    Ru.521 (5  mg/kg, i.p.; 2  h before modeling) administration in mice. H&E staining showing Intratracheal and LP conditions in control and BAS mice at 7th day. Scale bars indicate 200  μm and 50  μm.

    RU.521 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Nov 26;22(1):566.  [Abstract]

    RU.521 (5 mg/kg; i.p.; daily) in mice. The fluorescence intensity of SFTPC and GSDMD is detected by immunofluorescence (bar  =  100 μm).

    RU.521 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Jan 14;S1097-2765(22)01217-5.  [Abstract]

    Effects of cGAS inhibition on [Ca2+]i elevation in HeLa cells induced by ssDNA or dsDNA fragment transfection (2 μg/mL, 6 h). RU.521 (20 μM; 4 h before imaging) is added 4 h before imaging.

    RU.521 purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2023 Jan 15:373:62-75.  [Abstract]

    RU.521 (2.4 μM) significantly reduces the elevation of cGAS and STING triggered by ZnONPs in BEAS-2B cells.

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    製品説明

    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 0.7 μM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS)[1].

    IC50 & Target

    IC50: 0.7 μM (dsDNA)[1]
    Cellular Effect
    Cell Line Type Value Description References
    H69AR IC50
    32.9 μM
    Compound: 3; RU-521
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    Inhibition of human cGAS expressed in THP1-Dual cells transfected with HT-DNA assessed as suppression of lipofectamine 2000:ds-DNA complex induced activation of cGAS incubated for 1 hr by Quanti-luc reagent based assay
    		[PMID: 34044539]
    THP1-Dual CC50
    38.4 μM
    Compound: 3; RU-521
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Cytotoxicity against human THP1-Dual cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    		[PMID: 34044539]
    体外実験

    RU.521 (0.1 nM-1000 μM; 72 h) suppresses dsDNA-induced signaling in macrophage cells[1].
    RU.521(0-100 μM; 24 h) selectively inhibits cGAS-mediated signaling[1].

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

    RU.521 関連抗体
    体内実験

    RU.521 (5 mg/kg ; i.p. once) reduces symptoms from sepsis in mice[2].

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

    Animal Model: Male 8-week-old male mice with LPS injection[2]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection; 5 mg/kg once
    Result: Increased cardiac function and reduced the inflammatory responses, oxidative stress and apoptosis in hearts of mice.
    分子量

    415.23

    分子式

    C19H12Cl2N4O3
    CAS 番号
    Appearance

    Solid

    SMILES

    O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5
    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 : 83.33 mg/mL (200.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4083 mL 12.0415 mL 24.0830 mL
    5 mM 0.4817 mL 2.4083 mL 4.8166 mL
    10 mM 0.2408 mL 1.2042 mL 2.4083 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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:  50% PEG300    50% Saline

      Solubility: 2 mg/mL (4.82 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    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

    純度: 99.95%

    COA (251 KB) HNMR (259 KB) RP-HPLC (266 KB) LCMS (90 KB)

    取扱説明書 (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.4083 mL 12.0415 mL 24.0830 mL 60.2076 mL
    5 mM 0.4817 mL 2.4083 mL 4.8166 mL 12.0415 mL
    10 mM 0.2408 mL 1.2042 mL 2.4083 mL 6.0208 mL
    15 mM 0.1606 mL 0.8028 mL 1.6055 mL 4.0138 mL
    20 mM 0.1204 mL 0.6021 mL 1.2042 mL 3.0104 mL
    25 mM 0.0963 mL 0.4817 mL 0.9633 mL 2.4083 mL
    30 mM 0.0803 mL 0.4014 mL 0.8028 mL 2.0069 mL
    40 mM 0.0602 mL 0.3010 mL 0.6021 mL 1.5052 mL
    50 mM 0.0482 mL 0.2408 mL 0.4817 mL 1.2042 mL
    60 mM 0.0401 mL 0.2007 mL 0.4014 mL 1.0035 mL
    80 mM 0.0301 mL 0.1505 mL 0.3010 mL 0.7526 mL
    100 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6021 mL
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    RU.521 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • 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:

    RU.5212262452-06-0RU320521RU 320521RU-320521Cyclic GMP-AMP SynthasecGASsignaling pathwayoxidative stressinflammatoryInhibitorinhibitorinhibit

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    製品名:
    RU.521
    製品番号:
    HY-114180
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