1. Cell Cycle/DNA Damage Autophagy Apoptosis
  2. PERK Autophagy Apoptosis
  3. GSK2606414

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.

For research use only. We do not sell to patients.

GSK2606414 Chemical Structure

GSK2606414 Chemical Structure

CAS No. : 1337531-36-8

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 131 In-stock
Solution
10 mM * 1 mL in DMSO USD 131 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 156 In-stock
50 mg USD 420 In-stock
100 mg USD 648 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 73 publication(s) in Google Scholar

Top Publications Citing Use of Products

66 Publications Citing Use of MCE GSK2606414

WB
IF
Cell Viability Assay

    GSK2606414 purchased from MedChemExpress. Usage Cited in: NPJ Parkinsons Dis. 2023 Mar 7;9(1):35.  [Abstract]

    Co-application of 100 nM GSK2606414 or 100 nM KIRA8 with 10 nM thapsigargin for 48 h significantly mitigate thapsigargin-induced cell death of both the Ctrl and iKO (inducible knockout) midbrain DAergic neurons of mice.

    GSK2606414 purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Nov 15;e0328222.  [Abstract]

    GSK2606414 (10 µM; 24 h) or C16 (1 µM; 24 h) substantially decreases MGF110-7L-induced phosphorylation of PERK, PKR, and eIF2a in 3D4/21 cells (transfected with an empty Flag vector or a MGF110-7LFlag-expressing vector).

    GSK2606414 purchased from MedChemExpress. Usage Cited in: Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01442-18.  [Abstract]

    Extracellular tachyzoites are treated with 1 µM Thapsigargin in the presence of different concentrations of GSK2606414 (PERKi) as indicated or incubated with vehicle (DMSO) for 1 hour.

    GSK2606414 purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Apr 9;13(4):e0194310.  [Abstract]

    HeLa cells are treated with Tun in the absence or presence of PERK kinase inhibitor GSK2606414 (1 μM) with DMSO as the control. Total cell lysates are prepared, normalized for total protein and immunoblotting of indicated proteins ASB7, CHOP and ATF4 for 6 h in HeLa cells.

    GSK2606414 purchased from MedChemExpress. Usage Cited in: Neuroscience. 2018 Apr 1;375:34-48.  [Abstract]

    Western blot analysis of p-eIF2α in axotomized DRG spot cultures pretreated with or without GSK2606414 (10 μM) 30 min prior to axotomy. Cells are collected 1 h after axotomy.

    GSK2606414 purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.  [Abstract]

    Effects of GSK2606414 on the levels of Plasmodium eIF2a phosphorylation 24 hr after 75 mg/kg GSK2606414 treatment of mice infected with asynchronized P. berghei ANKA (A) and 48 hr after 2 mM GSK2606414 treatment of asynchronized P. falciparum 3D7 parasites in culture (B).

    GSK2606414 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2016 Nov 11;480(2):166-172.  [Abstract]

    An inhibitor of PERK, GSK2606414, is examined. Treatment and immunostaining are performed as per. Note that large CD63 and Rab7 positive vesicles appeared during ER stress when cells are pre-treated with GSK2606414.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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)

    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.

    In Vivo

    GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice[1].

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

    Molecular Weight

    451.44

    Formula

    C24H20F3N5O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=C2C(N(C)C=C2C3=CC4=C(N(C(CC5=CC=CC(C(F)(F)F)=C5)=O)CC4)C=C3)=NC=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (221.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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%Tween80

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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.91%

    References
    Animal Administration
    [1]

    Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with -200 mm3 tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated. Results are represented as percent inhibition on completion of dosing, which is 100[1-(average growth of drug-treated population)/(average growth of vehicle-treated control population)]. Statistical analysis is performed using a two-tailed t test.

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

    References

    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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2151 mL 11.0757 mL 22.1513 mL 55.3783 mL
    5 mM 0.4430 mL 2.2151 mL 4.4303 mL 11.0757 mL
    10 mM 0.2215 mL 1.1076 mL 2.2151 mL 5.5378 mL
    15 mM 0.1477 mL 0.7384 mL 1.4768 mL 3.6919 mL
    20 mM 0.1108 mL 0.5538 mL 1.1076 mL 2.7689 mL
    25 mM 0.0886 mL 0.4430 mL 0.8861 mL 2.2151 mL
    30 mM 0.0738 mL 0.3692 mL 0.7384 mL 1.8459 mL
    40 mM 0.0554 mL 0.2769 mL 0.5538 mL 1.3845 mL
    50 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1076 mL
    60 mM 0.0369 mL 0.1846 mL 0.3692 mL 0.9230 mL
    80 mM 0.0277 mL 0.1384 mL 0.2769 mL 0.6922 mL
    100 mM 0.0222 mL 0.1108 mL 0.2215 mL 0.5538 mL
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    GSK2606414 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    GSK2606414
    Cat. No.:
    HY-18072
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