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Merck
CN

S8822

Sigma-Aldrich

SB-525334

≥98% (HPLC), solid, ALK5 inhibitor

别名:

6-[2--丁基-5-(6-甲基吡啶-2-基)-1H-咪唑-4-基]-喹喔啉

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About This Item

经验公式(希尔记法):
C21H21N5
分子量:
343.42
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

产品名称

SB-525334, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

solid

颜色

yellow

溶解性

DMSO: ≥20 mg/mL

创始人

GlaxoSmithKline

储存温度

2-8°C

SMILES字符串

Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4nccnc4c3)C(C)(C)C

InChI

1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)

InChI key

DKPQHFZUICCZHF-UHFFFAOYSA-N

应用

SB-525334已被用于研究TGFβ1介导的人滋养细胞分化。7

生化/生理作用

SB-525334在肾近端小管细胞中可阻断TGFβ1诱导的Smad2/3的激活。4 SB-525334可降低TGFβ1的敏感性,从而通过逆转肺动脉压而有益于肺动脉高血压。5 SB-525334可降低子宫平滑肌瘤等间充质肿瘤的发生率和大小。6
SB-525334是一种ALK5/I型TGFβ-R激酶抑制剂。
SB-525334是一种有效的激活素受体样激酶(ALK5)/I型TGFβ-受体激酶抑制剂,其 IC50 = 14.3 nM。

特点和优势

该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处

储存分类代码

11 - Combustible Solids

WGK

WGK 3

个人防护装备

dust mask type N95 (US), Eyeshields, Faceshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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访问文档库

Eugene T Grygielko et al.
The Journal of pharmacology and experimental therapeutics, 313(3), 943-951 (2005-03-17)
SB-525334 (6-[2-tert-butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline) has been characterized as a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). The compound inhibited ALK5 kinase activity with an IC(50) of 14.3 nM and was approximately 4-fold less potent
Matthew Thomas et al.
The American journal of pathology, 174(2), 380-389 (2009-01-01)
Mutations in the gene for the transforming growth factor (TGF)-beta superfamily receptor, bone morphogenetic protein receptor II, underlie heritable forms of pulmonary arterial hypertension (PAH). Aberrant signaling via TGF-beta receptor I/activin receptor-like kinase 5 may be important for both the
Neel I Nissen et al.
Cancers, 14(3) (2022-02-16)
The use of novel tools to understand tumour-fibrosis in pancreatic ductal adenocarcinoma (PDAC) and novel anti-fibrotic treatments are highly needed. We established a pseudo-3D in vitro model including humane pancreatic fibroblasts (PFs) and pancreatic cancer-associated fibroblasts (CAFs) in combination with
Nicholas J Laping et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 13(10), 3087-3099 (2007-05-17)
Transforming growth factor beta (TGF-beta), which generally stimulates the growth of mesenchymally derived cells but inhibits the growth of epithelial cells, has been proposed as a possible target for cancer therapy. However, concerns have been raised that whereas inhibition of
Hiroyuki Higashiyama et al.
Experimental and molecular pathology, 83(1), 39-46 (2007-02-06)
Activin receptor-like kinase 5 (ALK5) is a type I receptor of transforming growth factor (TGF)-beta. ALK5 inhibition has been reported to attenuate the tissue fibrosis including pulmonary fibrosis, renal fibrosis and liver fibrosis. To elucidate the inhibitory mechanism of ALK5

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