Protein Inhibitors - LY 364947 (CAS: 396129-53-6)

LY 364947 (CAS: 396129-53-6)

Catalog #：EBC51138

Biological Activity

Synonyms

HTS466284, TbetaR-I Inhibitor

Chemical Name

4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline

Application

LY 364947 is a selective ATP-competitive inhibitor of TGF-β Receptor I kinase

CAS Number

396129-53-6

Purity

≥98.0%

Molecular Weight

272.31

Molecular Formula

C₁₇H₁₂N₄

SMILES

N1C=C(C(=N1)C1=NC=CC=C1)C1=CC=NC2=C1C=CC=C2

Target & IC50

TGF-β Receptor I kinase : IC50 = 51 nM
RIPK2: IC50 = 0.11 μM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	3.6724 ml	18.3621 ml	36.7242 ml
5 mM	0.7345 ml	3.6724 ml	7.3448 ml
10 mM	0.3672 ml	1.8362 ml	3.6724 ml
50 mM	0.0734 ml	0.3672 ml	0.7345 ml

Solubility
DMSO: 27.2 mg/mL (100 mM)

Product Description

LY 364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase). Studies of mouse fibroblasts show that LY 364947 inhibits cellular growth and transcription activation via TGF-β Receptor I kinase inhibition. In addition, TGF-β Receptor I kinase is responsible for fibroblast proliferation and the accumulation of astrocytes around the fibrotic scar when injury occurs to cells. In vitro studies report that in the presence of LY 364947 the amount of reactive astrocytes at the lesion site is also reduced. Furthermore, studies show that LY 364947 strongly effects intraplug vasculature by increasing the extravasation of Dextran (sc-218165). LY 364947 is an inhibitor of eIF2 alpha, MLTK, p38 alpha and TGF β RII.