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H-151

H-151
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Purity:99.52%
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H-151

Catalog No. T5674Cas No. 941987-60-6
H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.
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Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$47In Stock
10 mg$72In Stock
25 mg$148In Stock
50 mg$296In Stock
100 mg$452In Stock
500 mg$987In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Product Introduction

Bioactivity
Description
H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.
In vitro
METHODS: Mouse monocyte macrophage RAW264.7 was treated with H-151 (0.25-2 μM) for 1 h, and then stimulated with rmCIRP (1 μg/mL) for 24 h. The level of IFN-β was measured by ELISA.
RESULTS: IFN-β was dose-dependently reduced in the culture supernatant of cells pretreated with H-151, which inhibited eCIRP-induced activation of STING in vitro. [1]
METHODS: Human monocytes THP-1 were treated with H-151 (0.5 μM) for 2 h, and the expression levels of target proteins were measured by Western Blot.
RESULTS: H-151 inhibited the phosphorylation of TBK1, and H-151 effectively inhibited the activation of hsSTING. [2]
In vivo
METHODS: To assay in vivo activity, H-151 (750 nmol, 200 μL) was administered intraperitoneally to Trex1-/- Ifnb1Δβ-luc/Δβ-luc reporter mice once daily for seven days.
RESULTS: When administered for one week, H-151 showed significant efficacy in Trex1-/- mice expressing a bioluminescent IFNβ reporter gene. [2]
METHODS: To test the role in cisplatin-induced acute kidney injury (AKI), H-151 (7 mg/kg) was administered intraperitoneally to C57BL/6J mice with cisplatin-induced AKI three times a day.
RESULTS: H-151 treatment significantly ameliorated cisplatin-induced renal injury, as evidenced by improvement in renal function, renal morphology, and renal inflammation.H-151 may be a potential therapeutic agent for the treatment of AKI, possibly by inhibiting STING-mediated inflammation and mitochondrial damage. [3]
Chemical Properties
Molecular Weight279.34
FormulaC17H17N3O
Cas No.941987-60-6
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
5% DMSO+95% Saline: 6.25 mg/mL (22.37 mM, precipitation)
Ethanol: 14.08 mg/ml (50.42 mM)
DMSO: 55 mg/mL (196.89 mM)
Solution Preparation Table
DMSO/5% DMSO+95% Saline
1mg5mg10mg50mg
1 mM3.5799 mL17.8993 mL35.7987 mL178.9933 mL
5 mM0.7160 mL3.5799 mL7.1597 mL35.7987 mL
10 mM0.3580 mL1.7899 mL3.5799 mL17.8993 mL
20 mM0.1790 mL0.8950 mL1.7899 mL8.9497 mL
DMSO
1mg5mg10mg50mg
50 mM0.0716 mL0.3580 mL0.7160 mL3.5799 mL
100 mM0.0358 mL0.1790 mL0.3580 mL1.7899 mL

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