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Postion:Product Catalog >Biochemical Engineering>Inhibitors>protein tyrosine kinase>PP121
PP121
  • PP121

PP121 NEW

Price $51 $78 $156
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: PP121 CAS No.: 1092788-83-4
Purity: 99.67% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NamePP121
DescriptionPP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
Cell ResearchFor western blot analysis, cells are grown in 12-well plates and treated with PP-121 at the indicated concentrations or vehicle (0.1% DMSO). Treated cells are lysed, lysates are resolved by SDS-PAGE, transferred to nitrocellulose and blotted. For cell proliferation assays,cells are grown in 96-well plates are treated with PP-121 at 4-fold dilutions (10 μM - 0.040 μM) or vehicle (0.1% DMSO). After 72 hours cells are exposed to Resazurin sodium salt (22 μM) and fluorescence is quantified. IC50 values are calculated using Prism software. For proliferation assays involving single cell counting, non-adherent cells are plated at low density (3–5% confluence) and treated with PP-121 (2.5 μM) or vehicle (0.1% DMSO). Cells are diluted into trypan blue daily and viable cells counted using a hemocytometer. For apoptosis and cell cycle analysis, cells are treated with the indicated concentration of PP-121 or vehicle (0.1% DMSO) for 24–72 hours. Cells are either stained live with AnnexinV-FITC or fixed with ethanol and stained with propidium iodide. Cell populations are separated using a FacsCalibur flow cytometer; data is collected using CellQuest Pro software and analyzed with either ModFit or FlowJo Software.(Only for Reference)
Kinase AssayKinase assays: Purified kinase domains are incubated with PP-121 at 2- or 4-fold dilutions over a concentration range of 1 nM-50 μM or with vehicle (0.1% DMSO) in the presence of 10 μM ATP, 2.5 μCi of γ-32P-ATP and substrate. Reactions are terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane is then washed 5–6 times to remove unbound radioactivity and dried. Transferred radioactivity is quantitated by phosphorimaging and IC50 values are calculated by fitting the data to a sigmoidal doseresponse using Prism software.
In vivoIn glioma cell lines (U87 and LN229), PP-121 (0.04-10 μM) dose-dependently inhibited Akt, p70S6K and S6 phosphorylation, and PP-121 (0.04-10 μM) inhibited the proliferation of a range of tumor cells by directly inhibiting PI3Ks and mTOR. PP-121 induced cell arrest at G0/G1 phase in LN220, U87 and Seg1 cells. PP-121 (0.08-20 μM) inhibited v-Src-induced tyrosine phosphorylation in NIH3T3 cells transformed with v-Src (Thr338). Acting on NIH3T3 cells transformed with v-Src(Thr338), PP-121 (2.5 μM) restored the staining of actin fibers. PP-121 (40 nM) inhibited Ret autophosphorylation when applied to TT thyroid cancer cells expressing Ret mutation 35 of the C634W oncogene.PP-121 inhibited the proliferation of TT thyroid cancer cells (IC50: 50 nM). When acting on human umbilical vein endothelial cells, PP-121 inhibited VEGF-stimulated cell proliferation (IC50: 41 nM).
Storagekeep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationH2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (6.26 mM)
DMSO : 60 mg/mL (187.9 mM)
KeywordsSrc | Platelet-derived growth factor receptor | mTOR | PDGFR | PP 121 | VEGFR | PP-121 | inhibit | Apoptosis | Inhibitor | Mammalian target of Rapamycin | PP121 | Vascular endothelial growth factor receptor
Inhibitors RelatedStavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride
Related Compound LibrariesAnti-Colorectal Cancer Compound Library | Apoptosis Compound Library | Glycolysis Compound Library | Reprogramming Compound Library | Antidepressant Compound Library | Tyrosine Kinase Inhibitor Library | Antioxidant Compound Library | Anti-Prostate Cancer Compound Library | Cytoskeletal Signaling Pathway Compound Library | Oxidation-Reduction 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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