JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].

JAK3-IN-9 (compound 11i) shows high selective inhibition of JAK3 with IC 50 value of 1.7 nM [1]. Cell Viability Assay Cell Line: PBMCs [1] Concentration: 1 μM Incubation Time: 30 min Result: Showed preferential inhibition of JAK3 [1].

JAK3-IN-9 (compound 11i) (Female Lewis rats; 3, 10 and 30 mg/kg; Oral gavage once daily for 20 days) can selectively inhibit JAK3 cytokine signaling in the primary cells [1]. JAK3-IN-9 (Male DBA1j of 8 to 12-weeks old mice; 1mg/kg, Intravenous injection, Single administration) shows high AUC of 2104 μg/ml, extends t 1/2 to 2.56 h and good oral bioavailability of 48% [1]. JAK3-IN-9 (30 mg/kg; Oral gavage once daily for 20 days) suppress paw swelling in a dose-dependent manner with ED 50 value of 10 mg/kg [1]. Animal Model: Male DBA1j (8 to 12-weeks old) mice; Female Lewis rats [1]. Dosage: 1, 3, 10 and 30 mg/kg Administration: I.V, Single administration; IG, once daily for 20 days. Result: Showed anti-arthritis activity in the CIA mice model [1].