LY-364947 NEW
| Price | $59 | $75 | $146 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: LY-364947 | CAS No.: 396129-53-6 |
| Purity: 99.96% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | LY-364947 |
| Description | LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I. |
| 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. |
| 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. |
| Storage | Powder: -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. |
| Keywords | HTS-466284 | Transforming growth factor beta receptors | Inhibitor | inhibit | LY-364947 | HTS 466284 | TGF-β Receptor | LY364947 |
| Inhibitors Related | Monocrotaline | SB-431542 | Oditrasertib | Emodin | Chromenone 1 | Pirfenidone | A 83-01 | Galunisertib | Alantolactone | LY294002 |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | TGF-beta/Smad Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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