H-151 |
| Katalog-Nr.GC34610 |
H-151 ist ein potenter, selektiver und kovalenter Antagonist von STING, der sowohl in Zellen als auch in vivo eine bemerkenswerte inhibitorische AktivitÄt aufweist.
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Cas No.: 941987-60-6
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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