2241300-50-3
2241300-50-3 結構式
基本信息
1,2,5-Oxadiazol-3-amine, 4-[1-(2-methyl-1H-benzimidazol-6-yl)-1H-imidazo[4,5-c]pyridin-2-yl]-
物理化學性質
常見問題列表
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CDK8 0.61 nM (IC 50 ) |
CDK19 4.28 nM (IC 50 ) |
GSK3α 76.67 nM (IC 50 ) |
GSK3β 63.06 nM (IC 50 ) |
STAT5
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AS2863619 (1 μM; 22 hours; mouse CD4 + T cells) treatment suppresses serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples.
Western Blot Analysis
| Cell Line: | Mouse CD4 + T cells |
| Concentration: | 1 μM |
| Incubation Time: | 22 hours |
| Result: | Suppressed serine phosphorylation of the PSP motif of STAT5b to ~40% while enhancing tyrosine phosphorylation in the C-terminal domain to ~160% of control-treated samples. |
AS2863619 (30 mg/kg; oral administration; daily; for 2 weeks; mice) treatment after sensitization with 2,4-dinitrofluorobenzene (DNFB) dampens the degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreases ratios of interferon-γ + (IFN-γ + ) cells in a skin contact hypersensitivity model, when compared with vehicle-treated control mice. T reg depletion before the elicitation of the secondary response abolishes AS2863619-induced suppression. KLRG1 + Foxp3 + T cells are specifically increased in DNFB sensitized AS2863619-treated mice.
| Animal Model: | Mice with DNFB-induced contact skin hypersensitivity |
| Dosage: | 30 mg/kg |
| Administration: | Oral administration; daily; for 2 weeks |
| Result: | The degree of the secondary response, with milder infiltration of inflammatory cells into the skin and decreased ratios of interferon-γ + (IFN-γ + ) cells. |