| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 130 mg/mL (287.97 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.86 mM), Sonication is recommended.
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| 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 | Aceglutamide | Hemin | Urea | Guanidine hydrochloride | Hydroxychloroquine | Metronidazole | Formamide | Paeonol | Naringin | Daraxonrasib | Alginic acid |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Reprogramming Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | Autophagy Compound Library | Anti-Viral Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Oxidation-Reduction Compound Library |
United States
