H-151

SKU: orb1301596

Description

H-151 is a potent, selective, and covalent STING antagonist that acts by binding to Cys91 and inhibiting its palmitoylation. This compound is a valuable research tool for investigating STING-driven autoinflammatory diseases in both in vivo and in vitro experimental models.

Research Area

Immunology & Inflammation, Neuroscience

Key Properties

• CAS Number: 941987-60-6
• MW: 279.34
• Purity: >98%
• Formula: C₁₇H₁₇N₃O
• SMILES: CCc1ccc(NC(=O)Nc2c[nH]c3ccccc23)cc1
• Target: STING
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• Target IC50:
  MEF cells:138 nM|HFF cells:134.4 nM|BMDMs:109.6 nM
• 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. 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.
• 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. 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

STING, Stimulator of Interferon Genes, TBK1, phosphorylation, TMEM173, autoinflammatory, ERIS, H151, H-151, H 151, Inhibitor, inhibit, MPYS, palmitoylatio, MITA

Compound Identifiers

PubChem CID

7616033