1. Cell Cycle/DNA Damage
  2. PERK

GSK2606414 

Cat. No.: HY-18072 Purity: 99.18%
Data Sheet SDS 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 $109 In-stock
5 mg $99 In-stock
10 mg $130 In-stock
50 mg $350 In-stock
100 mg $540 In-stock
200 mg $900 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

    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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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GSK2606414 is an orally available and selective PERK inhibitor with an IC50 of 0.4 nM.

    IC50 & Target

    IC50: 0.4 nM (PERK)

    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].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Animal Administration
    [1]

    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 using the following equation: tumor volume (mm3) = (length × width2)/2. 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
    Molecular Weight

    451.44

    Formula

    C₂₄H₂₀F₃N₅O

    CAS No.

    1337531-36-8

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

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

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

    Purity: 99.18%

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    Inquiry Information

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