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Merck
CN

L6293

Sigma-Aldrich

LY-364947

≥98% (HPLC)

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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About This Item

经验公式(希尔记法):
C17H12N4
分子量:
272.30
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.77

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


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Xuning Shen et al.
Cell death & disease, 11(1), 65-65 (2020-01-29)
Colorectal cancer (CRC) is one of the leading causes of cancer death worldwide, and metastasis is the major cause of CRC-related mortality. Transforming growth factor-beta (TGF-β) has a central role not only in the regulation of the normal colon but
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
Lishen Shan et al.
Molecular medicine reports, 18(2), 2088-2096 (2018-06-20)
The present study aimed to investigate the effect of epigallocatechin gallate (EGCG) on airway inflammation in mice with bronchial asthma, and the regulatory mechanism of transforming growth factor (TGF)‑β1 signaling pathway, so as to provide theoretical basis for research and
Yu Liang et al.
Scientific reports, 6, 29479-29479 (2016-07-06)
The role of transforming growth factor-β (TGF-β) signaling in cancer progression is still under debate. To determine the function of TGF-β signaling in bladder cancer progression, we conditionally knocked out the Tgfbr2 in mouse model after a N-butyl-N-4-hydroxybutyl Nitrosamine induced
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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