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Merck

L6293

LY-364947

≥98% (HPLC), Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor, powder

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:
396129-53-6
Poids moléculaire :
272.30
UNSPSC Code:
51111800
PubChem Substance ID:
24724526
NACRES:
NA.77
MDL number:
MFCD00800758

Nom du produit

LY-364947, ≥98% (HPLC)

SMILES string

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

InChI key

IBCXZJCWDGCXQT-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Gene Information

human ... TGFBR1(7046)

Catégories apparentées

Biochem/physiol Actions

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.
Transforming Growth Factor-β Type I receptor kinase (ALK5) inhibitor

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

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

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Certificats d'analyse (COA)

Lot/Batch Number
0000523219
0000523219
0000331153
0000331153
0000220801

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Consulter la Bibliothèque de documents

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
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
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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