Product Details
| Product Name:
GSK2606414 |
CAS No.:
1337531-36-8 |
| Purity:
98.63% |
Supply Ability:
10g |
| Release date:
2025/07/16 |
Product Introduction
Bioactivity
| Name | GSK2606414 |
| Description | GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice. |
| In vitro | METHODS: S1-M1-80 vector and S1-M1-80 sgABCG2 cells were treated with GSK2606414 (0.1, 1, 3, 10, 30, 100 μM, 72 hours), and cytotoxicity was determined by MTT assay.
RESULTS GSK2606414 showed dose-dependent cytotoxic effects on both cell lines. [2]
METHODS: N2A cells were treated with GSK2606414 (0.5, 1 μM, 24 hours) and high glucose (30 mM), cells were lysed, and Western blot analysis was performed.
RESULTS N2A cells treated with GSK2606414 reduced the phosphorylation of eIF2α in cells and significantly reduced p-PERK levels in a dose-dependent manner, and GSK2606414 could inhibit the PERK/p-eIF2α/ATF4/CHOP signaling axis. [3] |
| In vivo | METHODS: GSK2606414 (50, 150 mg/kg, oral, twice a day, 21 days) was used to treat mice bearing subcutaneous pancreatic human BxPC3 tumors and the effect on tumor growth was observed.
RESULTS GSK2606414 inhibited tumor growth in a dose-dependent manner, with the tumor growth inhibition rates of 20% and 59% at the two doses, respectively. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (110.76 mM), Sonication is recommended.
|
| Keywords | Protein kinase R-like endoplasmic reticulum kinase | PKR-like endoplasmic reticulum kinase | PERK | Inhibitor | inhibit | GSK-2606414 | GSK2606414 | GSK 2606414 | eIF-2AK3 (PERK) | eIF-2AK2 (PKR) | eIF-2AK1 (HRI) | Autophagy | Apoptosis |
| Inhibitors Related | Stavudine | Cysteamine hydrochloride | Dextran sulfate sodium salt (MW 4500-5500) | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Tributyrin | Paeonol | Naringin | L-Ascorbic acid sodium salt | Alginic acid | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Osteogenesis Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical 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.
You may like
-
-
CAS:31828-68-9
$0.00 / 1removed
-
CAS:1278553-16-4
$293.00 / 1mg
Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States