Product Details
| Product Name:
GNF4877 |
CAS No.:
2041073-22-5 |
| Purity:
99.40% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | GNF4877 |
| Description | GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation. |
| In vitro | Concentrations of GNF4877 (0.1 μM, 0.3 μM) well below the EC50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. High glucose concentrations and glucokinase activators (GKAs) increase Ca2+ signaling in β-cells, and increase intracellular Ca2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Finally, increasing intracellular Ca2+ with glibenclamide or Bay K8644 shows additive activity with GNF4877. |
| In vivo | In double transgenic RIP-DTA male mice, GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control. |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4.17 mg/mL (8.43 mM), Sonication and heating are recommended.
|
| Keywords | GSK-3 | inhibit | Glycogen synthase kinase-3 | Glycogen synthase kinase 3 | GNF4877 | GNF-4877 | Inhibitor | Dual specificity tyrosine regulated kinase | GNF 4877 | Dual specificity tyrosine phosphorylation regulated kinase | DYRK |
| Inhibitors Related | Harmine | PHA-767491 | Cromolyn sodium | GSK 3 Inhibitor IX | CHIR-99021 | AT7519 | 5-Bromoindole | 4-Chloro-2'-bromoacetophenone | SNS-032 | GSK-3 Inhibitor 5 | MeBIO | 1-Azakenpaullone |
| Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer 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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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$127.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States