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S4317

Sigma-Aldrich

SB 431542 hydrate

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

Sinónimos:

4-(5-Benzol[1,3]dioxol-5-yl-4-pyrldin-2-yl-1H-imidazol-2-yl)-benzamide hydrate, 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-benzamide hydrate, 4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]-benzamide hydrate

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About This Item

Fórmula empírica (notación de Hill):
C22H16N4O3 · xH2O
Número de CAS:
301836-41-9
Peso molecular:
384.39 (anhydrous basis)
Número MDL:
MFCD11045982
Código UNSPSC:
51111800
ID de la sustancia en PubChem:
24724609
NACRES:
NA.77

Nombre del producto

SB 431542 hydrate, ≥98% (HPLC), powder

Nivel de calidad

100

Ensayo

≥98% (HPLC)

Formulario

powder

solubilidad

DMSO: soluble 10 mg/mL
H2O: insoluble

emisor

GlaxoSmithKline

temp. de almacenamiento

−20°C

cadena SMILES

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

Clave InChI

WQUIJVKNPYBZOF-UHFFFAOYSA-N

Aplicación

SB-431542 was used to study the correlation of platelet-derived growth factor receptor B expression and TGF-β pathway activation in colorectal tumor cells. It was used to study the role of TGF-β signaling in modulation of extracellular matrix and myoblast differentiation.

Acciones bioquímicas o fisiológicas

Potent and selective inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors.
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.

Características y beneficios

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Información legal

Sold for research purposes under agreement from Glaxo­Smith­Kline

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

Eyeshields, Gloves, type N95 (US)

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Certificados de análisis (COA)

Lot/Batch Number
0000420154
0000420154
0000411212
0000411212
0000410269

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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)
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
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
Yu Zhang et al.
Frontiers in cell and developmental biology, 8, 573028-573028 (2020-10-13)
BMP2 is a critical factor that is involved in the processes of embryo implantation and uterine decidualization. The expression of cyclooxygenase (COX) and subsequent prostaglandin E2 (PGE2) production are critical for successful pregnancy. However, it is not clear whether BMP2
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
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