1. Immunology/Inflammation
  2. STING
  3. 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.

For research use only. We do not sell to patients.

H-151 Chemical Structure

H-151 Chemical Structure

CAS No. : 941987-60-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 90 In-stock
50 mg USD 360 In-stock
100 mg USD 550 In-stock
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Customer Review

Based on 55 publication(s) in Google Scholar

Top Publications Citing Use of Products

54 Publications Citing Use of MCE H-151

IF

    H-151 purchased from MedChemExpress. Usage Cited in: Toxicol Lett. 2022 Nov 29;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).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    In Vitro

    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.

    In Vivo

    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.

    Molecular Weight

    279.34

    Formula

    C17H17N3O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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
    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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    V2

    In Vivo:

    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

    Animal weight
    (per animal)

    g

    Dosing volume
    (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.
    Purity & Documentation

    Purity: 99.86%

    References

    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

    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.

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    Product Name:
    H-151
    Cat. No.:
    HY-112693
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