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> H-151 [941987-60-6]

H-151 [941987-60-6]

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Referentie HY-112693-50mg

Formaat : 50mg

Merk : MedChemExpress


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]
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]
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.

H-151 Related Antibodies

Solvant et solubilité
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.

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.
Pureté et documentation
Références

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