2. Immunology/Inflammation
  3. STING
  4. H-151

H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease.

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CAS 番号 : 941987-60-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 在庫あり
Solution
10 mM * 1 mL in DMSO USD 66 在庫あり
Solid
5 mg $60 在庫あり
10 mg $90 在庫あり
50 mg $360 在庫あり
100 mg $550 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 138 publication(s) in Google Scholar

H-151 関連抗体

Top Publications Citing Use of Products

顧客検証

IF
WB
Cell Proliferation/Viability Assay
RT-PCR

    H-151 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 18:e2401634.  [Abstract]

    H-151 (750 nmol in 200 µL PBS with 5% Tween-80) suppresses radiation-induced phosphorylation of TBK1 and IRF3 in the colons of C57BL/6J mice.

    H-151 purchased from MedChemExpress. Usage Cited in: Small. 2024 Mar;20(9):e2307448.  [Abstract]

    H-151 (1-10 μM; 24 h) dose-dependently reduces 223Ra (3.7 kBq/mL; 48 h)-induced cytotoxicity in LLC cells.

    H-151 purchased from MedChemExpress. Usage Cited in: Small. 2024 Mar;20(9):e2307448.  [Abstract]

    H-151 (1 μM; 24 h) significantly attenuates 223Ra (3.7 kBq/mL; 48 h)-induced upregulation of NLRP3 expression while increasing the cleaved GSDMD/GSDMD ratio in LLC cells.

    H-151 purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2023 Jan 15:373:172-183.  [Abstract]

    H-151 (H151; 750 nM/mice; i.p.; every 12 h for 72 h) significantly restores inflammatory cell infiltration and ECM deposition in the mice with EsA (fig K), and decreases collagen fiber streaks (blue-stained area) (fig M).

    H-151 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Oct 5;33(10):2076-2089.e9.  [Abstract]

    FHs 74 Int cells were pretreated with 1 μM H-151 or 4 μM C-170 for 2 h and then exposed to 10 Gy ionizing radiation. IFNb expression was examined by qPCR 2 h after irradiation.

    H-151 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2021 May 15;81(10):2714-2729.  [Abstract]

    RT-qPCR analysis of CCL5, CXCL10, ISG15 and IFI44 expression in HOC7 with depletion of STING by STING inhibition (1 μM H151) for 24 hours (E) or si-STING (100μM) for 48 hours (F)

    • 生物活性

    • 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

    H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease[1].

    IC50 & Target

    STING[1]
    Cellular Effect
    Cell Line Type Value Description References
    BMDM IC50
    502.8 μM
    Compound: 24; H-151
    Cytotoxicity against mouse BMDM cells assessed as cell viability
    Cytotoxicity against mouse BMDM cells assessed as cell viability
    		[PMID: 35635952]
    HFF IC50
    134.4 μM
    Compound: 24; H-151
    Cytotoxicity against HFF cells assessed as cell viability
    Cytotoxicity against HFF cells assessed as cell viability
    		[PMID: 35635952]
    MEF IC50
    109.6 μM
    Compound: 24; H-151
    Cytotoxicity against MEF cells assessed as cell viability
    Cytotoxicity against MEF cells assessed as cell viability
    		[PMID: 35635952]
    体外実験

    H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells[1].
    H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells[1].
    H-151 (1 μM; 3 h) suppresses hsSTING palmitoylation[1].

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

    H-151 関連抗体
    体内実験

    H-151 (750 nmol per mouse; a single i.p.) markedly reduces systemic cytokine responses in CMA-treated mice[1].
    H-151 (750 nmol per mouse; i.p. daily for 7 d) exhibits notable efficacy in Trex1 / mice that expressed a bioluminescent IFNβ reporter[1].
    H-151 (750 nmol per mouse; i.p.) reaches effective systemic levels, displays a short half-life in the serum and forms an adduct to mmSTING in wild-type mice[1].

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

    279.34

    分子式

    C17H17N3O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CNC2=C1C=CC=C2)NC3=CC=C(CC)C=C3
    輸送条件

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

    DMSO : 100 mg/mL (357.99 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 3.5799 mL 17.8993 mL 35.7987 mL
    5 mM 0.7160 mL 3.5799 mL 7.1597 mL
    10 mM 0.3580 mL 1.7899 mL 3.5799 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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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）

    C1

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    体積 （開始）

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    濃度 （終了）

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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:  5% DMSO    5% Tween-80    90% PBS

      Solubility: 2.5 mg/mL (8.95 mM); Suspended solution; Need ultrasonic

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (7.45 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.
    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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    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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: 99.86%

    COA (249 KB) HNMR (205 KB) RP-HPLC (148 KB) MS (85 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, 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 3.5799 mL 17.8993 mL 35.7987 mL 89.4967 mL
    5 mM 0.7160 mL 3.5799 mL 7.1597 mL 17.8993 mL
    10 mM 0.3580 mL 1.7899 mL 3.5799 mL 8.9497 mL
    15 mM 0.2387 mL 1.1933 mL 2.3866 mL 5.9664 mL
    20 mM 0.1790 mL 0.8950 mL 1.7899 mL 4.4748 mL
    25 mM 0.1432 mL 0.7160 mL 1.4319 mL 3.5799 mL
    30 mM 0.1193 mL 0.5966 mL 1.1933 mL 2.9832 mL
    40 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2374 mL
    50 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7899 mL
    60 mM 0.0597 mL 0.2983 mL 0.5966 mL 1.4916 mL
    80 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
    100 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
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    H-151 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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:

    H-151941987-60-6H151H 151STINGStimulator of Interferon GenesTMEM173MITAERISMPYSTBK1phosphorylationpalmitoylatioautoinflammatoryInhibitorinhibitorinhibit

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    製品名:
    H-151
    製品番号:
    HY-112693
    数量:
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