1652629-23-6
Chemical Structure
GSK484
- CAS. Nr.: 1652629-23-6
- Formula:C27H31N5O3
- Molecular Weight:473.57
IUPAC Name: ((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone
InChIKey: BDYDINKSILYBOL-WMZHIEFXSA-N
SMILES: O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3C(N=C(C(N4CC5CC5)=CC6=C4C=CC=C6)N3C)=C2
Biological Activity: GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8+ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions[1][2][3][4][5][6].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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GSK484 | 99.14% | GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8+ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions. | ||||||||||||||||||||
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- [1]. Zhu X, et al. Ferrostatin-1 reduces the inflammatory response of rheumatoid arthritis by decreasing the antigen presenting function of fibroblast-like synoviocytes. J Transl Med. 2025;23(1):280. Published 2025 Mar 6. [Content Brief]
- [2]. Zhu X, et al. Ferroptosis Induces gut microbiota and metabolic dysbiosis in Collagen-Induced arthritis mice via PAD4 enzyme. Gene. 2025;936:149106. [Content Brief]
- [3]. Tran H, et al. Critical Role of Protein Arginine Deiminase 4 in Mast Cell Extracellular Trap Formation Leading to Neuropathic Pain in Sickle Mice[J]. Blood, 2017, 130: 439.
- [4]. Mand M, et al. Peptidylarginine deiminase 4 deficiency alleviates hypoxia/reoxygenation-induced cardiomyocyte injury. PLoS One. 2025;20(9):e0330864. Published 2025 Sep 10. [Content Brief]
- [5]. Ansari J, et al. Regulating Neutrophil PAD4/NOX-Dependent Cerebrovasular Thromboinflammation. Int J Biol Sci. 2023;19(3):852-864. Published 2023 Jan 9. [Content Brief]
- [6]. Xie K, et al. The PAD4 inhibitor GSK484 diminishes neutrophil extracellular trap in the colon mucosa but fails to improve inflammatory biomarkers in experimental colitis. Biosci Rep. Published online May 20, 2025. [Content Brief]
Keywords
