BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
IC50&Target
JAK3
STAT5
体外研究
BD750 inhibits human T cell proliferation stimulated either by anti-CD3/anti-CD28 mAbs or by alloantigen in a dose-dependent manner with IC50 values of 1.1 ± 0.2 μM and 1.3 ± 0.2 μM respectively.
BD750 also inhibits ConA, PMA/ionomycine or alloantigen-induced mouse T cell proliferation and PHA or PMA/ionomycine-induced human T cell proliferation.
BD750 (5 or 20 μM) inhibits the LPS-induced JAK-STAT5 signaling in DC.
Western Blot Analysis
Cell Line:
Purified immature DCs.
Concentration:
1, 5 or 20 μM.
Incubation Time:
12 h.
Result:
Had fewer small dendrites and smaller clusters than typical mDCs (5 or 20 μM).
At a higher dose significantly reduced the levels of LPS-stimulated IL-6, IL-12, TNF-α, IL-1β and IL-23 production by DCs.
体内研究
BD750 can induce tolerogenic dendritic cells (tolDC) and their function in experimental autoimmune encephalitis (EAE) in mice.
Animal Model:
Female C57BL/6 mice (10 wks old, 19-21 g).
Dosage:
20 μM.
Administration:
IV, treated DC on d 7, 11 and 15 post the first PTX injection (dpi 7, 11 and 15).
Result:
Significantly reduced the frequency of Th1 and Th17 cells and increased the percentage of Tregs compared with mice receiving PBS.
分子式
C14H13N3Os
分子量
271.34
CAS号
892686-59-8
运输条件
Room temperature in continental US; may vary elsewhere.