Description
A cell-permeable indole-3-propanamide immunosuppressant that is shown to selectively inhibit the kinase activity of JAK3 (by 81% and 36% at 90 and 30 µM, respectively) over that of JAK2 (by 29% and 0% at 90 and 30 µM, respectively) and reduce JAK1/3-dependent phosphorylations of Akt, STAT5a/b, and Erk1/2 in IL-2-stimulated CTL-L2 cells, but not JAK1/2-dependent STAT1 phosphorylation in INF-γ-stimulated U266 cultures. Reported to inhibit ConA-stimulated murine splenocytes and PHA-stimulated human PBL proliferation (IC50 = 17 and 25 µM, respectively) in vitro and be efficacious in ameliorating delayed hypersensitivity reaction in mice (by ~78% with a daily oral dose of 50 mg/kg) and in prolonging the survival of heart transplant-recipient rats (by >3-fold with 60 mg/kg/day, p.o.) in vivo.
Abbr
JAK3 Inhibitor VII, AD412(JAK3)
Alias
JAK-3, JAK3_HUMAN, JAKL, L-JAK, LJAK
Storage
+2 centigrade to +8 centigrade
Synonyms
JAK-3, JAK3_HUMAN, JAKL, L-JAK, LJAK
Molecular Formula
C23H20ClN3O
Chemical Name
N-(Pyridin-4-yl)-3-[1-(4-chlorobenzyl)indol-3-yl]-propanamide