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> GSK2606414 [1337531-36-8]

GSK2606414 [1337531-36-8]

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Référence HY-18072-10mg

Conditionnement : 10mg

Marque : MedChemExpress

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Description

GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.

IC50 & Target[1]

EIF2AK3 (PERK)

0.4 nM (IC50)

EIF2AK1 (HRI)

420 nM (IC50)

EIF2AK2 (PKR)

696 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
<0.03 μM
Compound: 1, GSK2606414
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
[PMID: 24900593]
A549 IC50
<0.03 μM
Compound: 38, GSK2606414
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells after 2 hrs by Western blotting
[PMID: 22827572]
Caco-2 CC50
70.35 μM
Compound: GSK2606414
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
Caco-2 IC50
0.25 μM
Compound: GSK2606414
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
L929 IC50
0.4 nM
Compound: 40; GSK'414
Anti-neprotic activity in mouse L929 cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr by SYTOX Green dye based fluorescence assay
Anti-neprotic activity in mouse L929 cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr by SYTOX Green dye based fluorescence assay
[PMID: 31622096]
MEF IC50
7.3 nM
Compound: 40; GSK'414
Anti-neprotic activity in mouse MEF cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr in presence of z-VAD by SYTOX Green dye based fluorescence assay
Anti-neprotic activity in mouse MEF cells assessed as reduction in TNF-induced necroptosis and measured every 1 hr in presence of z-VAD by SYTOX Green dye based fluorescence assay
[PMID: 31622096]
In Vitro

GSK2606414 inhibits PERK activation in cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GSK2606414 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 90.91 mg/mL (201.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2151 mL 11.0757 mL 22.1513 mL
5 mM 0.4430 mL 2.2151 mL 4.4303 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% HPMC/0.2% Tween-80 in Saline water

    Solubility: 3.33 mg/mL (7.38 mM); Suspended solution; Need ultrasonic
Pureté et documentation
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