S8822
SB-525334
≥98% (HPLC), solid, ALK5 inhibitor
别名:
6-[2-叔-丁基-5-(6-甲基吡啶-2-基)-1H-咪唑-4-基]-喹喔啉
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关于此项目
经验公式（希尔记法）:
C21H21N5
CAS Number:
分子量:
343.42
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
Product Name
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
相关类别
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
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
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
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
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
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
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