H-151

Catalog No.S6652 Batch:S665203

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Technical Data

Formula

C17H17N3O
Molecular Weight 279.34 CAS No. 941987-60-6
Solubility (25°C)* In vitro DMSO 56 mg/mL (200.47 mM)
Ethanol 14 mg/mL (50.11 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description H-151 is a highly potent and covalent antagonist of STING that has noteworthy inhibitory activity both in human cells and in vivo.
Targets
STING [1]
In vivo

After intraperitoneal administration, H-151 reachs effective systemic levels, displays a short half-life in the serum and formed an adduct to mmSTING. Notably, pretreatment of H-151 markedly reduces systemic cytokine responses in CMA-treated mice. Moreover, H-151 exhibits notable efficacy in Trex1−/− mice that expressed a bioluminescent IFNβ reporter, when administered for one week.[1]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    FLDMs

  • Concentrations

    25 µM

  • Incubation Time

    12 h

  • Method

    Cells were treated with indicated concentrations of drug.
Animal Study:

[2]
  • Animal Models

    C57BL/6J mice

  • Dosages

    750 nM

  • Administration

    i.p.

Selleck's H-151 has been cited by 26 publications

STING orchestrates the neuronal inflammatory stress response in multiple sclerosis [ Cell, 2024, 187(15):4043-4060.e30] PubMed: 38878778
TRPM2-mediated feed-forward loop promotes chondrocyte damage in osteoarthritis via calcium-cGAS-STING-NF-κB pathway [ J Adv Res, 2024, S2090-1232(24)00499-5] PubMed: 39505144
Inhibiting autophagy enhanced mitotic catastrophe-mediated anticancer immune responses by regulating the cGAS-STING pathway [ Cancer Lett, 2024, 586:216695] PubMed: 38325769
Blockade of the mitochondrial DNA release ameliorates hepatic ischemia-reperfusion injury through avoiding the activation of cGAS-Sting pathway [ J Transl Med, 2024, 22(1):796] PubMed: 39198913
Nilotinib boosts the efficacy of anti-PDL1 therapy in colorectal cancer by restoring the expression of MHC-I [ J Transl Med, 2024, 22(1):769] PubMed: 39143573
Polystyrene microplastics induce pulmonary fibrosis by promoting alveolar epithelial cell ferroptosis through cGAS/STING signaling [ Ecotoxicol Environ Saf, 2024, 277:116357] PubMed: 38677073
Interleukin-1β promotes human metapneumovirus replication via activating the cGAS-STING pathway [ Virus Res, 2024, 343:199344] PubMed: 38431054
Aryl hydrocarbon receptor suppresses STING-mediated type I IFN expression in triple-negative breast cancer [ Sci Rep, 2024, 14(1):5731] PubMed: 38459088
H-151, a Selective STING Inhibitor, Has Potential as a Treatment for Neovascular Age-Related Macular Degeneration [ Invest Ophthalmol Vis Sci, 2024, 65(8):16] PubMed: 38980271
Mitochondrial DNA-Activated cGAS-STING Signaling in Environmental Dry Eye [ Invest Ophthalmol Vis Sci, 2024, 65(4):33] PubMed: 38648040

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.