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AS1517499

AS1517499

产品编号 T4476   CAS 919486-40-1

AS1517499 是可透过血脑屏障的STAT6磷酸化抑制剂,IC50为 21 nM。

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AS1517499 Chemical Structure
AS1517499, CAS 919486-40-1
规格 价格/CNY 货期 数量
1 mg ¥ 297 现货
2 mg ¥ 421 现货
5 mg ¥ 728 现货
10 mg ¥ 1,120 现货
25 mg ¥ 1,730 现货
50 mg ¥ 2,580 现货
100 mg ¥ 3,790 现货
500 mg ¥ 8,170 现货
1 mL * 10 mM (in DMSO) ¥ 759 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: AS1517499 (T4476)
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纯度: 98.7%
纯度: 98.31%
纯度: 98.27%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM
靶点活性 STAT6:21 nM
体外活性 AS1517499 shows potent STAT6 inhibition with an IC50 value of 21 nM. AS1517499 also inhibits IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM and without influencing T-helper cell 1 (Th1) differentiation induced by IL-12. AS1517499 selectively inhibits Th2 differentiation without affecting Th1 differentiation[1]. In cultured human BSM cells, IL-13 (100 ng/mL) causes a phosphorylation of STAT6 and an upregulation of RhoA, a monomeric GTPase responsible for Ca2+ sensitization of smooth muscle contraction: both events are inhibited by co-incubation with AS1517499 (100 nM)[2] .
体内活性 In BALB/c mice that are actively sensitized and repeatedly challenged with ovalbumin antigen, an increased IL-13 level in bronchoalveolar lavage fluids and a phosphorylation of STAT6 in bronchial tissues are observed after the last antigen challenge. These mice have an augmented BSM contractility to acetylcholine together with an up-regulation of RhoA in bronchial tissues. Intraperitoneal injections of AS1517499 (10 mg/kg) 1 hour before each ovalbumin exposure almost completely inhibits both the antigen-induced up-regulation of RhoA and BSM hyperresponsiveness[2].
细胞实验 Normal human BSM cells (hBSMCs) are maintained in SmBM medium supplemented with 5% fetal bovine serum, 0.5 ng/mL human epidermal growth factor (hEGF), 5 μg/mL insulin, 2 ng/mL human fibroblast growth factor-basic (hFGFb), 50 μg/mL gentamicin, and 50 ng/mL amphotericin B. Cells are maintained at 37°C in a humidified atmosphere (5% CO2), fed every 48 to 72 hours, and passaged when cells reached 90 to 95% confluence. Then the hBSMCs (passages 7-9) are seeded in 6-well plates and 8-well chamber slides at a density of 3,500 cells/cm2 and, when 80 to 85% confluence observed, cells are cultured without serum for 24 hours before addition of recombin is ant human IL-13. AS1517499 (100 nM) or its vehicle (0.3% DMSO) is treated 30 minutes before the addition of IL-13 (100 ng/mL). In some experiments, AS1517499 is treated 0 (co-incubation), 3, or 12 hours after the addition of IL-13. In another series of experiments, a selective Rho-kinase inhibitor Y-27632 (1 μM) or its vehicle (0.3% DMSO) is also applied 15 minutes before the IL-13 application. At the indicated time after the IL-13 treatment, cells are washed with PBS, immediately collected, and disrupted with 1× SDS sample buffer (250 μL/well), and used for Western blot analyses[2] .
动物实验 Mice[2]
分子量 397.86
分子式 C20H20ClN5O2
CAS No. 919486-40-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 35 mg/mL

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TargetMol Library Books参考文献

1. Nagashima S, et al. Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg Med Chem. 2007 Jan 15;15(2):1044-55. 2. Am J Respir Cell Mol Biol. 2009 Nov;41(5):516-24.

TargetMol Library Books文献引用

1. Qin R, Wang T, He W, et al.Jak2/STAT6/c-Myc pathway is vital to the pathogenicity of Philadelphia-positive acute lymphoblastic leukemia caused by P190BCR-ABL.Cell Communication and Signaling.2023, 21(1): 27. 2. Tao Y, Xu L, Liu X, et al.Chitosan-coated artesunate protects against ulcerative colitis via STAT6-mediated macrophage M2 polarization and intestinal barrier protection.International Journal of Biological Macromolecules.2023: 127680.
3-O-Methylgallic acid STAT3-IN-1 Atractylenolide I Kurarinone S3I-201 Cirsilineol Stafib-2 HO-3867

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 干细胞分化化合物库 抗癌细胞代谢库 抗肺癌化合物库 抗癌化合物库 抗肥胖化合物库 抗衰老化合物库 细胞凋亡化合物库 免疫/炎症分子化合物库 成骨分子库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AS1517499 919486-40-1 JAK/STAT signaling Stem Cells STAT AS-1517499 inhibit AS 1517499 Inhibitor inhibitor

 

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