所有图片(1)
别名:
4-(4′-苯氧基苯胺)-6,7-二甲氧基喹唑啉, 6,7-二甲氧基-N-（4-苯氧基苯基）-4-喹唑啉, SKI-1, Src-l1
经验公式（希尔记法）:
C22H19N3O3
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质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
white
溶解性
DMSO: >10 mg/mL
储存温度
2-8°C
SMILES字符串
COc1cc2ncnc(Nc3ccc(Oc4ccccc4)cc3)c2cc1OC
InChI
1S/C22H19N3O3/c1-26-20-12-18-19(13-21(20)27-2)23-14-24-22(18)25-15-8-10-17(11-9-15)28-16-6-4-3-5-7-16/h3-14H,1-2H3,(H,23,24,25)
InChI key
DMWVGXGXHPOEPT-UHFFFAOYSA-N
应用
Src抑制剂-1可用于Src激酶介导的细胞信号转导研究。
生化/生理作用
Src抑制剂-1是一种有效的、竞争性的双重位点（ATP和肽结合）Src激酶抑制剂。Src抑制剂-1是Src激酶抑制的“金标准”之一。研究已经显示通过Src-I1与PP1或PP2一起使用可抑制Src家族激酶。Src抑制剂-1是酪氨酸激酶Src家族的选择性竞争性抑制剂（分别对于Src和Lck的IC50为44nM和88nM）。Src抑制剂-1可以更高的浓度抑制VEGFR2和c-fms酪氨酸激酶（IC50分别为0.32 μM和30 μM）。
除Src激酶外，一些Src抑制剂也可抑制Abl激酶、Lck、Csk和Yes蛋白的活性，因此研究人员正在探索将其作为可行的抗癌药物的可能性。
特点和优势
这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
WGK
WGK 3
Diane H Boschelli et al.
Journal of medicinal chemistry, 47(7), 1599-1601 (2004-03-19)
We previously reported that several 7-alkoxy-4-phenylamino-3-quinolinecarbonitriles were potent inhibitors of Src kinase activity. We disclose here a new highly efficient and versatile route to these compounds, which are also potent inhibitors of Abl kinase.
Changli Wei et al.
The Journal of clinical investigation, 129(5), 1946-1959 (2019-02-08)
Soluble urokinase plasminogen activator receptor (suPAR) is an immune-derived circulating signaling molecule that has been implicated in chronic kidney disease, such as focal segmental glomerulosclerosis (FSGS). Typically, native uPAR (isoform 1) translates to a 3-domain protein capable of binding and
Klaske M Schukken et al.
Life science alliance, 3(2) (2020-01-26)
Chromosomal instability (CIN) and aneuploidy are hallmarks of cancer. As most cancers are aneuploid, targeting aneuploidy or CIN may be an effective way to target a broad spectrum of cancers. Here, we perform two small molecule compound screens to identify
Lei Chen et al.
Phytomedicine : international journal of phytotherapy and phytopharmacology, 57, 72-83 (2019-01-23)
Periploca forrestii(PF) is mainly utilized for treatment of arthritis and traumatic injury historically. We had previously demonstrated that a fraction rich in cardiotonic steroids isolated from PF had the potential to facilitate wound healing. However, the exact material basis and
Yi-Fang Yang et al.
Oncogenesis, 9(8), 78-78 (2020-08-31)
Cholesterol is the major component of lipid rafts. Squalene synthase (SQS) is a cholesterol biosynthase that functions in cholesterol biosynthesis, modulates the formation of lipids rafts and promotes lung cancer metastasis. In this study, we investigated the lipid raft-associated pathway
商品
Src is the original member of a group of non-receptor protein-tyrosine kinases termed the Src family kinases (SFKs). Learn about the SFKs that, in humans, consist of eight members, a small group of atypical members, and two related kinases.
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