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Merck
CN

S4317

SB 431542 水合物

≥98% (HPLC), powder, inhibits activation of SMAD proteins

别名:

4-(5-苯并[1,3]二唑-5-基-4-吡啶-2-基-1H-咪唑-2-基)-苯甲酰胺 水合物, 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯甲酰胺 水合物, 4-[4-(3,4-亚甲二氧基苯基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯甲酰胺 水合物

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关于此项目

经验公式（希尔记法）:
C22H16N4O3 · xH2O
化学文摘社编号:
301836-41-9
分子量:
384.39 (anhydrous basis)
UNSPSC Code:
51111800
PubChem Substance ID:
24724609
NACRES:
NA.77
MDL number:
MFCD11045982
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

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产品名称

SB 431542 水合物, ≥98% (HPLC), powder

SMILES string

O.NC(=O)c1ccc(cc1)-c2nc(-c3ccc4OCOc4c3)c([nH]2)-c5ccccn5

InChI

1S/C22H16N4O3.H2O/c23-21(27)13-4-6-14(7-5-13)22-25-19(20(26-22)16-3-1-2-10-24-16)15-8-9-17-18(11-15)29-12-28-17;/h1-11H,12H2,(H2,23,27)(H,25,26);1H2

InChI key

WQUIJVKNPYBZOF-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

solubility

DMSO: soluble 10 mg/mL
H2O: insoluble

originator

GlaxoSmithKline

storage temp.

−20°C

Quality Level

100

相关类别

Application

SB-431542被用于研究结直肠肿瘤细胞中血小板衍生生长因子受体B表达与TGF-β途径激活的相关性。它被用于研究TGF-β信号传导在调节细胞外基质 和成肌细胞分化中的作用。

Biochem/physiol Actions

SB-431542可抑制TGF-β介导的SMAD蛋白活化、胶原和纤连蛋白表达、细胞增殖和细胞运动。它不抑制因血清或应激而激活的激酶，如ERK、p38或JNK。
转化生长因子-β超家族I型激活素受体样激酶（ALK）受体的有效和选择性抑制剂。

Features and Benefits

该化合物由 GlaxoSmithKline开发。想要浏览其他由制药公司开发的化合物以及已批准物/候选药物清单， 请单击此处。

Legal Information

根据Glaxo­Smith­Kline协议出售，用于研究目的

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000517761
0000517761
0000481104
0000481104
0000477529

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N J Laping et al.
Molecular pharmacology, 62(1), 58-64 (2002-06-18)
Transforming growth factor beta1 (TGF-beta1) is a potent fibrotic factor responsible for the synthesis of extracellular matrix. TGF-beta1 acts through the TGF-beta type I and type II receptors to activate intracellular mediators, such as Smad proteins, the p38 mitogen-activated protein
A Smad3 and TTF-1/NKX2-1 complex regulates Smad4-independent gene expression.
Isogaya K, Koinuma D, Tsutsumi S, et al.
Cell Research, 24(8), 994-1008 (2014)
Gareth J Inman et al.
Molecular pharmacology, 62(1), 65-74 (2002-06-18)
Small molecule inhibitors have proven extremely useful for investigating signal transduction pathways and have the potential for development into therapeutics for inhibiting signal transduction pathways whose activities contribute to human diseases. Transforming growth factor beta (TGF-beta) is a member of
Paola Bendinelli et al.
International journal of molecular sciences, 20(10) (2019-05-28)
Hepatocyte growth factor (HGF) and transforming growth factor β1 (TGFβ1) are biological stimuli of the micro-environment which affect bone metastasis phenotype through transcription factors, but their influence on the growth is scarcely known. In a xenograft model prepared with 1833
Douglas S Micalizzi et al.
The Journal of clinical investigation, 119(9), 2678-2690 (2009-09-04)
Inappropriate activation of developmental pathways is a well-recognized tumor-promoting mechanism. Here we show that overexpression of the homeoprotein Six1, normally a developmentally restricted transcriptional regulator, increases TGF-beta signaling in human breast cancer cells and induces an epithelial-mesenchymal transition (EMT) that
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Step-by-step culture protocols for neural stem cell culture including NSC isolation, expansion, differentiation and characterization.

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