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GNF-362 is an inositol triphosphate 3 kinase (ITPK) inhibitor (IC50s = 20, 9, and 19 nM for ITPKA, ITPKB, and ITPKC, respectively).1 It induces calcium influx in isolated mouse splenocytes (EC50 = 12 nM). In vivo, GNF-362 (10 and 25 mg/kg) reduces the number of thymic CD4+ T cells in mice. It also reduces inflammatory cell infiltration, joint erosion, and proteoglycan loss, in a rat model of antigen-induced arthritis when administered at a dose of 20 mg/kg.
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1. Inhibition of the inositol kinase Itpkb augments calcium signaling in lymphocytes and reveals a novel strategy to treat autoimmune disease. PLoS One 10(6), e0131071 (2015).