质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
ClC1=CC(CCNC2=NC=C(C(N)=O)C(NCC3=CC=CC=C3)=N2)=CC=C1O
InChI
1S/C20H20ClN5O2/c21-16-10-13(6-7-17(16)27)8-9-23-20-25-12-15(18(22)28)19(26-20)24-11-14-4-2-1-3-5-14/h1-7,10,12,27H,8-9,11H2,(H2,22,28)(H2,23,24,25,26)
InChI key
OZRMEKAUZBKTTC-UHFFFAOYSA-N
生化/生理作用
AS1517499 是一种有效的 STAT6(信号转导子和转录激活子 6)抑制剂(IC 50 = 21 nM,抑制 IL-4 依赖性报告基因活性),可选择性地阻止抗 CD3-和IL-4 诱导小鼠脾脏 T 细胞的辅助性 T 细胞 2 (Th2) 分化 (IC 50 = 2.3 nM),并且不影响抗 CD3和IL-12 诱导 Th1 分化。AS1517499的体内功效在各种免疫性疾病动物模型中得到证实,包括自身免疫性Graves病,抗原诱导的支气管过度收缩(10 mg / kg i.p.)。
AS1517499适度抑制RhoA(ras同源家族A)的表达。 RhoA蛋白的过表达与过敏性支气管哮喘有关。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Bioorganic & medicinal chemistry, 15(2), 1044-1055 (2006-10-31)
The STAT6 (signal transducers and activators of transcription 6) protein is activated by interleukin (IL)-4 and IL-13, and plays an important role in T-helper cell 2 (Th2) differentiation. STAT6 might therefore be an excellent therapeutic target for various allergic conditions
Science (New York, N.Y.), 352(6288), aad3018-aad3018 (2016-05-21)
Macrophages accumulate with glioblastoma multiforme (GBM) progression and can be targeted via inhibition of colony-stimulating factor-1 receptor (CSF-1R) to regress high-grade tumors in animal models of this cancer. However, whether and how resistance emerges in response to sustained CSF-1R blockade
The proximal STAT6 and NF-κB sites are responsible for IL-13-and TNF-α-induced RhoA transcriptions in human bronchial smooth muscle cells.
Pharmacological Research, 61(5), 466-472 (2010)
Cell death & disease, 7(12), e2506-e2506 (2016-12-03)
Signal transducer and activator of transcription 6 (STAT6) is involved in epithelial cell growth. However, little is known regarding the STAT6 phosphorylation status in Graves' disease (GD) and its role in thyroid epithelial cells (TECs). In this study, we found
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