L6293
LY-364947
≥98% (HPLC), Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor, powder
别名:
4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉, HTS 466284, 转化生长因子-β I型受体激酶抑制剂
登录 查看公司和协议定价
选择尺寸
关于此项目
经验公式（希尔记法）:
C17H12N4
化学文摘社编号:
分子量:
272.30
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.77
产品名称
LY-364947, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
c1ccc(nc1)-c2n[nH]cc2-c3ccnc4ccccc34
InChI
1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)
InChI key
IBCXZJCWDGCXQT-UHFFFAOYSA-N
基因信息
human ... TGFBR1(7046)
生化/生理作用
LY-364947 是转化生长因子-β I 型受体激酶（TGF-β RI，ALK5）的选择性 ATP 竞争性抑制剂，IC50 = 59 nM。它对相关激酶的效力要差得多，TGF-β RII 的 IC50 = 400 nM ，混合谱系激酶 7（MLK-7）（MAP 激酶信号途径中的激酶，与 TGF-β RII 密切相关）的 IC50 = 1400 nM。LY-364947 抑制 NIH 3T3 小鼠成纤维细胞中 TGF-β 依赖性细胞生长（IC50 = 81 nM）。
转化生长因子-β 型 I 受体激酶（ALK5）抑制剂
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
J Scott Sawyer et al.
Journal of medicinal chemistry, 46(19), 3953-3956 (2003-09-05)
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selectivity versus p38 MAP
Sheng-Ru Shiou et al.
The Journal of biological chemistry, 281(45), 33971-33981 (2006-09-09)
Metastasis is a primary cause of mortality due to cancer. Early metastatic growth involves both a remodeling of the extracellular matrix surrounding tumors and invasion of tumors across the basement membrane. Up-regulation of extracellular matrix degrading proteases such as urokinase
Khaled Nassar et al.
Experimental eye research, 123, 72-86 (2014-04-20)
This study evaluates the use of the TGF-β receptor 1 inhibitor LY-364947 (LY) to prevent proliferative vitreoretinopathy (PVR). For the in vitro experiments Human Tenon's Fibroblasts (HTFs) and retinal pigment epithelial (RPE) cells were treated with different concentrations of LY
Suzanne Vanhauwaert et al.
PloS one, 9(10), e109091-e109091 (2014-10-14)
The selection and validation of stably expressed reference genes is a critical issue for proper RT-qPCR data normalization. In zebrafish expression studies, many commonly used reference genes are not generally applicable given their variability in expression levels under a variety
Juswinder Singh et al.
Bioorganic & medicinal chemistry letters, 13(24), 4355-4359 (2003-12-04)
We describe the discovery, using shape-based virtual screening, of a potent, ATP site-directed inhibitor of the TbetaRI kinase, an important and novel drug target for fibrosis and cancer. The first detailed report of a TbetaRI kinase small molecule co-complex confirms
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持