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L6293

LY-364947

Name: LY-364947
Brand: SIGMA

≥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:

396129-53-6

分子量:

272.30

UNSPSC Code:

51111800

PubChem Substance ID:

24724526

NACRES:

NA.77

MDL number:

MFCD00800758

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

LY-364947, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

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

Gene Information

human ... TGFBR1(7046)

说明

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

历史批次信息供参考:

分析证书(COA)

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Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.

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Journal of medicinal chemistry, 49(6), 2138-2142 (2006-03-17)

Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus

Difference of TGF-β/Smads signaling pathway in epithelial-mesenchymal transition of normal colonic epithelial cells induced by tumor-associated fibroblasts and colon cancer cells.

Xiu-Lian Wang et al.

Molecular biology reports, 46(3), 2749-2759 (2019-03-06)

Tumor microenvironment (TME) crucially functions in tumor initiation and progression. Stroma-tumor interactions and cellular transdifferentiation are the prerequisite for tumor formation. Transforming growth factor-β (TGF-β), a major cytokine secreted by tumor-associated fibroblasts (TAFs) and cancer cells, is a crucial player

Epigallocatechin gallate improves airway inflammation through TGF‑β1 signaling pathway in asthmatic mice.

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

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货号	GTIN
L6293-5MG	04061833958728
L6293-25MG	04061832434094