H-151 |
Catalog No.GC34610 |
H-151 es un antagonista potente, selectivo y covalente de STING que tiene una notable actividad inhibitoria tanto en células como in vivo.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 941987-60-6
Sample solution is provided at 25 µL, 10mM.
H-151 is a low MW antagonist of STING, which blocks the activation-induced palmitoylation of STING, and exhibits significant inhibitory effects on STING signalling H-151 can be used in the study of autoinflammatory diseases[1-2].
H-151(1 µM; 6 h) exerts anti-psoriasis effect through inhibiting STING/NF-κB signalling[3]. H-151(2.5 µM; 24h) improved the inflammation of peripheral blood mononuclear cells and Coatomer complex I (COPI)-deficient cell lines in patients with COPA syndrome[4].
H-151(250 /500 mg/kg; on the shaved back and right ear;5days) displayed anti-inflammatory activity in both keratinocytes and immune cells, and decreased the severity of psoriatic response in vivo[3]. H-151 downregulated the expression of granzymes and the pro-inflammatory cytokines IL-1β, IL-6, IL-15, IL-23A, and IFN-γ, and induced a pro-resolution macrophage phenotypes in ALS patients [5]. Administration of H-151 alleviated pulmonary edema, hemorrhage, thickening of the alveolar septum and infiltration of inflammatory cells; DNA damage in pulmonary tissue; and disruption of intercellular junctions in LPS-induced ALI [6]. H-151(750 nmol; i.p) treatment preserves myocardial function 28 days after myocardial infarction (MI)[7].
References:
[1]. Haag SM, Gulen MF, et,al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. doi: 10.1038/s41586-018-0287-8. Epub 2018 Jul 4. PMID: 29973723.
[2]. Li J, Lu Y, et,al. Blocking cGAS/STING signaling protects against sepsis-associated acute liver injury. Int Immunopharmacol. 2022 Dec;113(Pt A):109276. doi: 10.1016/j.intimp.2022.109276. Epub 2022 Oct 15. PMID: 36252490.
[3]. Pan Y, You Y, et,al. The STING antagonist H-151 ameliorates psoriasis via suppression of STING/NF-κB-mediated inflammation. Br J Pharmacol. 2021 Dec;178(24):4907-4922. doi: 10.1111/bph.15673. Epub 2021 Oct 30. PMID: 34460100.
[4]. Steiner A, Hrovat-Schaale K, et,al. Deficiency in coatomer complex I causes aberrant activation of STING signalling. Nat Commun. 2022 Apr 28;13(1):2321. doi: 10.1038/s41467-022-29946-6. PMID: 35484149; PMCID: PMC9051092.
[5]. Zamiri K, Kesari S, et,al. Therapy of autoimmune inflammation in sporadic amyotrophic lateral sclerosis: Dimethyl fumarate and H-151 downregulate inflammatory cytokines in the cGAS-STING pathway. FASEB J. 2023 Aug;37(8):e23068. doi: 10.1096/fj.202300573R. PMID: 37436778; PMCID: PMC10619685.
[6]. Zhao J, Zhen N, et,al. NETs Promote Inflammatory Injury by Activating cGAS-STING Pathway in Acute Lung Injury. Int J Mol Sci. 2023 Mar 7;24(6):5125. doi: 10.3390/ijms24065125. PMID: 36982193; PMCID: PMC10049640.
[7]. Hu S, Gao Y, et,al. The selective STING inhibitor H-151 preserves myocardial function and ameliorates cardiac fibrosis in murine myocardial infarction. Int Immunopharmacol. 2022 Jun;107:108658. doi: 10.1016/j.intimp.2022.108658. Epub 2022 Mar 9. PMID: 35278833.
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