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Postion:Product Catalog >G007-LK
G007-LK
  • G007-LK

G007-LK NEW

Price $45 $64 $100
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: G007-LK CAS No.: 1380672-07-0
Purity: 98.62% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameG007-LK
DescriptionG007-LK is a selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
Cell ResearchCell lines: APC-mutant CRC cell lines COLO-320DM. Concentrations: ~0.2 μM. Method: For colony formation assays,cells are seeded at 500 cells/well in 2 mL medium.Cell line in triplicate wells is treated with either 0.06% DMSO or compound in 0.06% DMSO and incubated for up to 17 days or until colonies became sufficiently large to quantify.Colonies are stained with 200 μL of 12 mM 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide to each well for 1 h,and colony numbers are quantitated with a GelCount scanner at 1200 dpi resolution.
Kinase AssayTNKS1 and TNKS2 in vitro biochemical assays: G007-LK inhibitory activity at various doses (duplicates) is tested twice by TNKS1, TNSK2 Chemiluminescent Assay Kits, and the luminescence is measured.
Animal ResearchAnimal Models: Human APC –mutant CRC xenograft COLO-320DM. Formulation: 15% DMSO,17.5% Cremophor EL,8.75% ethanol,8.75% Miglyol 810N,50% PBS. Dosages: 20 mg/kg. Administration: intraperitoneal injection twice daily
In vitroG007-LK demonstrated anti-tumor efficacy in xenograft and genetically engineered CRC models. In the COLO-320DM model, it reduced levels of tankyrases 1 and 2, stabilized AXIN1 and AXIN2, and decreased β-catenin levels. G007-LK treatment increased the expression of KRT20 and TM4SF4 in COLO-320DM tumors. Administered at 20 mg/kg twice daily, G007-LK achieved a 61% inhibition of tumor growth. Additionally, it reduced Wnt/β-catenin signaling and cell proliferation in normal intestinal tissue.
In vivoG007-LK inhibits Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thus promoting β-catenin destabilization. In cell culture, it completely blocks ligand-driven Wnt/β-catenin signaling and demonstrates inhibition of approximately 50% in APC mutation-driven signaling across most CRC cell lines. G007-LK reduces mitotic COLO-320DM cells from 24% to 12% and S-phase HCT-15 cells from 28% to 18% at a concentration of 0.2 μM. It also inhibits colony formation in CRC cell lines COLO-320DM and SW403. Furthermore, G007-LK suppresses organ growth with an IC50 of 80 nM.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (175.5 mM)
KeywordsG007LK | Inhibitor | poly ADP ribose polymerase | G-007-LK | G007 LK | PARP | inhibit | G007-LK
Inhibitors RelatedUrea | 4'-Methoxychalcone | Wnt pathway activator 1 | CHIR-99021 | 3-Aminobenzamide | XAV-939 | Niraparib | Olaparib | Benzamide | Nefopam hydrochloride | OUL35 | Bisdemethoxycurcumin
Related Compound LibrariesAnti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Anti-Prostate Cancer Compound Library | NO PAINS Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max

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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