GSK2606414 [1337531-36-8]
Referência NB-64-15321-10mg
Tamanho : 10mg
Marca : Neo Biotech
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GSK2606414
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Catalog No. T2614 Copy Product Info
Purity: >99.99%
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.
Cas No. 1337531-36-8
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Purity:99.53%
Color:White to Yellow
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Product Information
GSK2606414 AI Summary
GSK2606414 exhibits a broad spectrum of bioactivities, including potent inhibition of various kinases such as YES1, WNK2, AXL, TRKB, TRKA, and PERK with IC50 values ranging from 154.0 nM to 3195.0 nM. It shows antitumor activity in human BxPC3 cell xenografts in nude mice, with tumor growth inhibition percentages of 20.0% to 59.0% at different dosages, and demonstrates high oral bioavailability from 62.0% to 100.0% across different animal models. The compound's half-life ranges from 2.5 to 10.6 hours, and its volume of distribution at steady state varies from 3.8 to 8.2 L/kg. In addition to its kinase inhibition, GSK2606414 exhibits antiviral activity against SARS-CoV-2, reducing virus-induced cytotoxicity in Caco-2 cells by 85.4% at 10 µM and showing an IC50 value of 250.0 nM. It also inhibits SARS-CoV-2 3CL-Pro protease and displays selectivity with a selectivity index greater than 100.0, with low toxicity indicated by a CC50 value of 70350.0 nM. The compound effectively inhibits RIPK1 (IC50 of 18.0 nM) and demonstrates strong anti-necrotic activity in mouse L929 and MEF cells with IC50 values of 0.4 nM and 7.3 nM, respectively. It also exhibits anti-inflammatory effects in a mouse model of systemic inflammatory response syndrome (SIRS). Additional bioactivities include inhibition of cytochrome P450 enzymes, thapsigargin-induced autophosphorylation of PERK in human A549 cells (IC50 < 30 nM), and Toxoplasma gondii GST-tagged IF2Kalpha (IC50 of 0.4 nM). It also shows selective inhibition among NEK enzymes and modest inhibition of human HDAC6. Overall, GSK2606414 is a promising candidate with diverse pharmacological activities including kinase inhibition, antiviral, antitumor, anti-inflammatory, and antiparasitic effects..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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. |
| Targets & IC50 | EIF2AK2 (PKR):696 nM, KIT (tyrosine kinase receptor):154 nM, EIF2AK3 (PERK):0.4 nM, ARPE-19 cells:1.7 µM, EIF2AK1 (HRI):420 nM, N2A cells:5.3 μM |
| 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] |
| Molecular Weight | 451.44 |
| Formula | C24H20F3N5O |
| Cas No. | 1337531-36-8 |
| Smiles | NC1=C2C(=CN(C)C2=NC=N1)C=3C=C4C(=CC3)N(C(CC5=CC(C(F)(F)F)=CC=C5)=O)CC4 |
| Relative Density. | 1.43 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight, 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.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.86 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
