BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.
BAY 61-3606 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HeLa cells
1 μM
1 hour
Inhibition of Syk significantly reduced Jedi-1 and MEGF10-mediated engulfment of microspheres
J Neurosci. 2012 Sep 19;32(38):13022-31
BM-derived macrophages
1 μM
60 min
Inhibited Syk phosphorylation, reduced inflammatory gene expression and phenotypic switching
Clin Transl Med. 2021 Jul;11(7):e463
human corneal epithelial cells (hTCEpi)
10 μM
48 h
BAY 61-3606 significantly reduced the expression of hBD2 and LL37 stimulated by F. solani or PAMPs (Zymosan or Zymosan Depleted) through inhibition of the Syk signaling pathway.
Invest Ophthalmol Vis Sci. 2017 May 1;58(5):2463-2472
vascular smooth muscle cells (VSMCs)
10 μM
48 h
To evaluate the time-dependent anti-proliferative effect of BAY61-3606 on VSMCs, results showed significant time-dependent inhibition.
Biol Res. 2017 Jan 18;50(1):1
vascular smooth muscle cells (VSMCs)
1, 5, 10, 20 μM
24 h
To evaluate the concentration-dependent anti-proliferative effect of BAY61-3606 on VSMCs, results showed significant concentration-dependent inhibition.
Biol Res. 2017 Jan 18;50(1):1
vascular smooth muscle cells (VSMCs)
10 μM
24 h
To evaluate the anti-proliferative effect of BAY61-3606 on VSMCs, results showed significant inhibition of cell proliferation.
Biol Res. 2017 Jan 18;50(1):1
UC mucosal myofibroblasts
0.01 –10 μg/mL
24 h
Evaluate the inhibitory effect of BAY-61-3606 on TNF-α-stimulated IL-6 and IL-8 release from UC myofibroblasts. BAY-61-3606 significantly reduced both IL-6 and IL-8 release with efficacy over 90%, but with weaker potency compared to TOP1210.
Inflamm Bowel Dis. 2016 Jun;22(6):1306-15
HT29 cells
0.1 –1000 ng/mL
2 h
Evaluate the inhibitory effect of BAY-61-3606 on IL-8 release from IL-1β-stimulated HT29 cells. BAY-61-3606 showed weak inhibitory effects with less than 50% inhibition.
Inflamm Bowel Dis. 2016 Jun;22(6):1306-15
Peripheral blood mononuclear cells
0.1 –1000 ng/mL
2 h
Evaluate the inhibitory effect of BAY-61-3606 on IL-8 release from LPS-stimulated PBMCs. BAY-61-3606 achieved a maximum inhibition of 83% with an IC50 of 607 nM.
Inflamm Bowel Dis. 2016 Jun;22(6):1306-15
BAY 61-3606 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice (Mus musculus, C57BL/6J)
Elastase-perfused AAA model
Intraperitoneal injection
50 mg/kg
3 times per week for 2 weeks (preventive treatment) or 1 week (therapeutic treatment)
Inhibited Syk activity, reduced AAA formation and progression, decreased inflammation and oxidative stress
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