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GSK2606414 [1337531-36-8]

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Referentie NB-64-15321-10mg

Formaat : 10mg

Merk : Neo Biotech

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GSK2606414

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Synonyms:

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

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.53%

Color:White to Yellow

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

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]

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.2151 mL	11.0757 mL	22.1513 mL	110.7567 mL
5 mM	0.4430 mL	2.2151 mL	4.4303 mL	22.1513 mL
10 mM	0.2215 mL	1.1076 mL	2.2151 mL	11.0757 mL
20 mM	0.1108 mL	0.5538 mL	1.1076 mL	5.5378 mL
50 mM	0.0443 mL	0.2215 mL	0.4430 mL	2.2151 mL
100 mM	0.0222 mL	0.1108 mL	0.2215 mL	1.1076 mL

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.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Please see Product Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal exp