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
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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
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
LY-364947, ≥98% (HPLC)
SMILES string
c1ccc(nc1)-c2n[nH]cc2-c3ccnc4ccccc34
InChI key
IBCXZJCWDGCXQT-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Gene Information
human ... TGFBR1(7046)
Biochem/physiol Actions
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
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
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
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
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
Natalia Dolgova et al.
Molecular neurobiology, 58(2), 855-866 (2020-10-11)
Demyelination and oligodendrocyte loss are characteristic changes in demyelinating disorders. Low-field magnetic stimulation (LFMS) is a novel transcranial neuromodulation technology that has shown promising therapeutic potential for a variety of neuropsychiatric conditions. The cellular and molecular mechanisms of magnetic stimulation
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