A selective PERK inhibitor
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GSK2606414

Item No. 17376

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]-ethanone
CAS Number
1337531-36-8
Molecular Formula
C24H20F3N5O
Formula Weight
451.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 2 mg/ml
λmax
210, 290 nm
SMILES
NC1=NC=NC2=C1C(C3=CC=C4C(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C3)=CN2C
InChi Code
InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)
InChi Key
SIXVRXARNAVBTC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $40

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    5 mg

    $171

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    10 mg

    $302

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    50 mg

    $918

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    Product Description

    GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM.1 It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.1 Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hetz, C., Chevet, E., and Harding, H.P. Targeting the unfolded protein response in disease. Nat. Rev. Drug Discov. 12(9), 703-719 (2013).