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
化学文摘社编号:
分子量:
343.42
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
SB-525334, ≥98% (HPLC)
SMILES string
Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4nccnc4c3)C(C)(C)C
InChI key
DKPQHFZUICCZHF-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
solid
color
yellow
solubility
DMSO: ≥20 mg/mL
originator
GlaxoSmithKline
storage temp.
2-8°C
Quality Level
Application
SB-525334已被用于研究TGFβ1介导的人滋养细胞分化。7
Biochem/physiol Actions
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。
Features and Benefits
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
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
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
Lindsay R Piraino et al.
Cells, 11(12) (2022-06-25)
The development of therapies to prevent or treat salivary gland dysfunction has been limited by a lack of functional in vitro models. Specifically, critical markers of salivary gland secretory phenotype downregulate rapidly ex vivo. Here, we utilize a salivary gland
Robert B Good et al.
BMC biomedical engineering, 1, 14-14 (2019-06-28)
Excessive extracellular matrix (ECM) deposition is a hallmark feature in fibrosis and tissue remodelling diseases. Typically, mesenchymal cells will produce collagens under standard 2D cell culture conditions, however these do not assemble into fibrils. Existing assays for measuring ECM production
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