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LY-364947

LY-364947
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
Catalog No. T2048Cas No. 396129-53-6
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Purity:99.96%
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LY-364947

Catalog No. T2048Cas No. 396129-53-6
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
5 mg$59In Stock
10 mg$75In Stock
25 mg$146In Stock
50 mg$268In Stock
100 mg$393In Stock
200 mg$589In Stock
500 mg$923In Stock
1 mL x 10 mM (in DMSO)$66In Stock
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Product Introduction

Bioactivity
Description
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.
Targets&IC50
TGFβRI:59 nM, MLK7K:1.4 μM, TGFβRII:0.4 μM, RIPK2:0.11 μM, CK1δ:0.22 μM
In vitro
Administering 1 mg/kg i.p. of LY364947 significantly enhances the LYVE-1-positive regions within the tumor tissues in a BxPC3 pancreatic cancer xenograft model. Similarly, 25 mg/kg i.p. of LY364947 markedly increases LYVE-1-positive areas in a chronic peritonitis mouse model, indicating accelerated lymphangiogenesis. Additionally, LY364947 (25 mg/kg) increases p-Akt levels and decreases nuclear Foxo3a in leukemia-initiating cells in mice infected with CML.
In vivo
At a concentration as low as 0.25 μM, LY364947 enhances the xVent2-lux BMP4 response in NMuMG cells by 30%. At 2 μM, it prevents TGF-β-induced epithelial-mesenchymal transition (EMT) in NMuMG cells. A 3 μM dose of LY364947, after 24 hours of treatment, induces the expression of Prox1 and LYVE-1 in nearly all HDLECs. LY364947 promotes the nuclear export of Foxo3a and is characterized by low Smad2/3 and high Akt phosphorylation levels in leukemia-positive cells. When co-cultured with OP-9 stromal cells, LY364947 (at concentrations <20 μM) inhibits the colony-forming ability of leukemia-initiating cells. Acting as an ATP-competitive, tight-binding inhibitor, LY364947 inhibits P-Smad3 phosphorylation through TGFβR-I kinase with a Ki of 28 nM and inhibits Smad2 phosphorylation in NMuMG cells in vivo with an IC50 of 135 nM.
Kinase Assay
The IC50 of LY-364947 at different enzyme concentrations are determined by the filter-binding assay. Typically, 40 μL reactions in 50 mM HEPES at pH 7.5, 1 mM NaF, 200 μM pKSmad3(-3), and 50 mM ATP containing a titration of each inhibitor with concentrations of 1600, 800, 400, 200, 100, 50, 25, and 0 nM are incubated at 30°C for 30 min. The IC50 is calculated using a nonlinear regression method with GraphPad Prism software. The binding type is determined by plotting the correlation between enzyme concentrations and IC50 values.
AliasLY 364947, HTS466284
Chemical Properties
Molecular Weight272.3
FormulaC17H12N4
Cas No.396129-53-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 7.5 mg/mL (27.54 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.6724 mL18.3621 mL36.7242 mL183.6210 mL
5 mM0.7345 mL3.6724 mL7.3448 mL36.7242 mL
10 mM0.3672 mL1.8362 mL3.6724 mL18.3621 mL
20 mM0.1836 mL0.9181 mL1.8362 mL9.1811 mL

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