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L6293

Sigma-Aldrich

LY-364947

≥98% (HPLC)

Synonyme(s) :

4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline, HTS 466284, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor

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About This Item

Formule empirique (notation de Hill):
C17H12N4
Numéro CAS:
Poids moléculaire :
272.30
Numéro MDL:
Code UNSPSC :
51111800
ID de substance PubChem :
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

c1ccc(nc1)-c2n[nH]cc2-c3ccnc4ccccc34

InChI

1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)

Clé InChI

IBCXZJCWDGCXQT-UHFFFAOYSA-N

Informations sur le gène

human ... TGFBR1(7046)

Actions biochimiques/physiologiques

LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges


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Consulter la Bibliothèque de documents

Juswinder Singh et al.
Bioorganic & medicinal chemistry letters, 13(24), 4355-4359 (2003-12-04)
We describe the discovery, using shape-based virtual screening, of a potent, ATP site-directed inhibitor of the TbetaRI kinase, an important and novel drug target for fibrosis and cancer. The first detailed report of a TbetaRI kinase small molecule co-complex confirms
Lishen Shan et al.
Molecular medicine reports, 18(2), 2088-2096 (2018-06-20)
The present study aimed to investigate the effect of epigallocatechin gallate (EGCG) on airway inflammation in mice with bronchial asthma, and the regulatory mechanism of transforming growth factor (TGF)‑β1 signaling pathway, so as to provide theoretical basis for research and
Yu Liang et al.
Scientific reports, 6, 29479-29479 (2016-07-06)
The role of transforming growth factor-β (TGF-β) signaling in cancer progression is still under debate. To determine the function of TGF-β signaling in bladder cancer progression, we conditionally knocked out the Tgfbr2 in mouse model after a N-butyl-N-4-hydroxybutyl Nitrosamine induced
Xiu-Lian Wang et al.
Molecular biology reports, 46(3), 2749-2759 (2019-03-06)
Tumor microenvironment (TME) crucially functions in tumor initiation and progression. Stroma-tumor interactions and cellular transdifferentiation are the prerequisite for tumor formation. Transforming growth factor-β (TGF-β), a major cytokine secreted by tumor-associated fibroblasts (TAFs) and cancer cells, is a crucial player
J Scott Sawyer et al.
Journal of medicinal chemistry, 46(19), 3953-3956 (2003-09-05)
Pyrazole-based inhibitors of the transforming growth factor-beta type I receptor kinase domain (TbetaR-I) are described. Examination of the SAR in both enzyme- and cell-based in vitro assays resulted in the emergence of two subseries featuring differing selectivity versus p38 MAP

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