1. Cell Cycle/DNA Damage
  2. PERK


Cat. No.: HY-18072 Purity: 99.38%
Handling Instructions

GSK2606414 is an orally available and selective 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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 131 In-stock
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 USD 1080 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

    GSK2606414 purchased from MCE. Usage Cited in: Neuroscience. 2018 Feb 10;375:34-48.

    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 MCE. Usage Cited in: Cell Host Microbe. 2017 Dec 13;22(6):766-776.e4.

    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 MCE. Usage Cited in: PLoS One. 2018 Apr 9;13(4):e0194310.

    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 MCE. Usage Cited in: Biochem Biophys Res Commun. 2016 Nov 11;480(2):166-172.

    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.

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    GSK2606414 is an orally available and selective 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]

    In Vivo

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

    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2215 mL 1.1076 mL 2.2151 mL
    Please refer to the solubility information to select the appropriate solvent.
    Animal Administration

    GSK2606414 is formulated in vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8).

    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.

    Molecular Weight




    CAS No.




    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    GSK2606414 is prepared in a solution with 0.5% hydroxypropyl methylcellulose and 0.1% Tween 80[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.


    Purity: 99.38%

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