JAK3-IN-9

JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research[1].

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Research Areas >> Inflammation/Immunology

JAK3:1.7 nM (IC50)

JAK3-IN-9 (compound 11i) shows high selective inhibition of JAK3 with IC50 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 t1/2 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 ED50 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].

[1]. Bahekar R, et al. Discovery of diaminopyrimidine-carboxamide derivatives as JAK3 inhibitors. Bioorg Chem. 2020 Jun;99:103851.