GNF362

GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC 50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC 50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+ -dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4]. In Vitro GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca 2+ responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes. GNF362 augments SOC responses following antigen receptor cross-linking, with an EC 50 of 12 nM in primary B or T lymphocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: A Lewis rat antigen-induced arthritis (rAIA) model Dosage: 6 or 20 mg/kg Administration: Orally administration; 6 or 20 mg/kg; twice daily; 21 days Result: Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively.

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