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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Cell Cycle>Rho inhibitor>EHop-016
EHop-016
  • EHop-016

EHop-016 NEW

Price $40 $67 $129
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: EHop-016 CAS No.: 1380432-32-5
Purity: 99.86% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameEHop-016
DescriptionEHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.
Cell ResearchMDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells (from ATCC) are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.(Only for Reference)
Kinase AssayRac Activity Assays: Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines (from ATCC). Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit.
In vitroEHop-016 significantly improves the survival rate of leukemia mice with KIT^D814V^ cells.
In vivoIn MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits the binding of active VAV2 to the Rac1 (G15A) mutant fusion protein, leading to a reduction in Rac-regulated cellular functions, including the formation of lamellipodia and cell migration. Due to compensatory mechanisms, the inhibition of Rac by EHop-016 results in increased activity of the closely related Rho GTPase RhoA. Additionally, EHop-016 suppresses the viability of MDA-MB-435 cells (IC50: 10 μM). EHop-016 also inhibits the growth induced by KITD814V in cells derived from SM and AML patients.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 50 mg/mL (116.13 mM), Sonication is recommended.
KeywordsRas | EHop016 | migration | Vav2 | Cdc42 | PAK1 | inhibit | EHop-016 | Rac3 | Rac1 | angiogenesis | Inhibitor
Inhibitors RelatedAdagrasib | (S)-AMG-510 | BI-2493 | CCG-257081 | Ketoconazole | SKLB-163 | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN | Sotorasib
Related Compound LibrariesFerroptosis Compound Library | Anti-Colorectal Cancer Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | GPCR 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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