GSK143 is an orally active, potent and selective syk inhibitor (pIC50 = 7.5 or IC50 = 31.6 nM) with good selectivity over 66 protein kinases, including ZAP-70 (pIC50 = 4.7 or IC50 = 20 μM). GSK143 effectively inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos cells (pIC50 = 7.1 or IC50 = 79.4 nM) and demonstrates in vivo efficacy in animal inflammatory disease models, including reverse Arthus passive reaction (10 & 30 mg/kg po. in rats), postoperative ileus (POI, 1, 3 or 10 mg/kg po. in mice), and chronic HDM-induced allergic airways inflammation (30 mg/kg/day po. in mice).
Orally active, potent and highly selective syk inhibitor with in vivo efficacy in animal inflammatory disease models.
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Hygroscopic
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11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
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Not applicable
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Not applicable
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Spleen tyrosine kinase (SYK) is a protein kinase involved in cell proliferation and the regulation of inflammatory pathways. Due to the increasing evidence that kinase inhibitors have potential as specific anti-inflammatory drugs, we have investigated the potential for SYK inhibition
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor
British Journal of Haematology, 182(6), 927-930 (2018)
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