CAS NO.：892686-59-8 Product Name：2-(1,3-Benzothiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-ol Synonyms：bd750;2-(1,3-benzothiazol-2-yl)-4,5,6,7-tetrahydro-2H-indazol-3-ol;STK241724;STK615824;ST50762732;2-benzothiazol-2-yl-2H-4,5,6,7-tetrahydroindazol-3-ol;2-(2-benzothiazoleyl)-4,5,6,7-tetrahydro-2h-indazol-3-ol;2-(1,3-benzothiazol-2-yl)-1,2,4,5,6,7-hexahydro-3H-indazol-3-one EINEC: Molecular Formula：C14H13N3OS Molecular Weight：271.337521314621
Target:
JAK3
STAT5
In Vivo
BD750 can induce tolerogenic dendritic cells (tolDC) and their function in experimental autoimmune encephalitis (EAE) in mice[2]. Animal Model: Female C57BL/6 mice (10 wks old, 19-21 g)[2]. 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.
In Vitro
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[1]. BD750 also inhibits ConA, PMA/ionomycine or alloantigen-induced mouse T cell proliferation and PHA or PMA/ionomycine-induced human T cell proliferation[1]. BD750 (5 or 20 μM) inhibits the LPS-induced JAK-STAT5 signaling in DC[2]. Western Blot Analysis[2] 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.
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Y Liu, et al. BD750, a benzothiazole derivative, inhibits T cell proliferation by affecting the JAK3/STAT5 signalling pathway. Br J Pharmacol. 2013 Feb;168(3):632-43.
[2]. Yan Zhou, et al. Tolerogenic dendritic cells induced by BD750 ameliorate proinflammatory T cell responses and experimental autoimmune encephalitis in mice. Mol Med. 2017 Oct;23:204-214.
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