JAK3抑制剂VII,AD412用途
JAK3抑制剂VII,AD412是一种细胞可渗透的吲哚-3-丙酰胺免疫抑制剂,与JAK2的活性(分别为29%和0)相比,选择性抑制JAK3激酶活性(分别在90和30μM时分别抑制81%和36%)。分别在90和30μM时产生%),并降低IL-2刺激的CTL-L2细胞中Akt,STAT5a / b和Erk1 / 2的JAK1和JAK3依赖性磷酸化,但不降低INF中JAK1 / 2依赖性STAT1磷酸化-γ刺激的U266培养物。据报道,JAK3抑制剂VII,AD412在体外抑制ConA刺激的鼠脾细胞和PHA刺激 JAK3 Inhibitor VII, AD412 is a cell-permeable indole-3-propanamide immunosuppressant that is shown to selectively inhibit JAK3 kinase activity (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 and JAK3-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. JAK3 Inhibitor VII, AD412 is reported to inhibit ConA-stimulated murine splenocytes and PHA-stimulated human PBL proliferation (IC|50|= 17 and 25 μM, respectively)|in vitro|.
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