GSK 2606414

Catalog # Availability Size / Price Qty
5107/10
5107/50
GSK 2606414 | CAS No. 1337531-36-8 | PERK Inhibitors
1 Image
Description: Potent and selective PERK inhibitor; orally bioavailable

Chemical 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

Purity: ≥99%

Product Details
Citations (16)
Reviews

Biological Activity

GSK 2606414 is a potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable.

Technical Data

M.Wt:
451.44
Formula:
C24H20F3N5O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
1337531-36-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes only under agreement from GlaxoSmithKline

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Citations for GSK 2606414

The citations listed below are publications that use Tocris products. Selected citations for GSK 2606414 include:

16 Citations: Showing 1 - 10

  1. Aorta- and liver-generated TMAO enhances trained immunity for increased inflammation via ER stress/mitochondrial ROS/glycolysis pathways.
    Authors: Yan Et al.
    JCI Insight  2023;8
  2. ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions
    Authors: Jeong Et al.
    Exp Mol Med  2023;
  3. Polyadenylated RNA and RNA-Binding Proteins Exhibit Unique Response to Hyperosmotic Stress.
    Authors: Jeffrey D Et al.
    Front Cell Dev Biol  2022;9:809859
  4. Saponin-based adjuvant-induced dendritic cell cross-presentation is dependent on PERK activation.
    Authors: Lisa G M Et al.
    Cell Mol Life Sci  2022;79:231
  5. The Unfolded Protein Response Sensor PERK Mediates Stiffness-Dependent Adaptation in Glioblastoma Cells.
    Authors: Yuanke Et al.
    Int J Mol Sci  2022;23
  6. LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells.
    Authors: Chong-Shan Et al.
    Autophagy  2022;18:204-222
  7. PERK signaling through C/EBPδ contributes to ER stress-induced expression of immunomodulatory and tumor promoting chemokines by cancer cells.
    Authors: Vishal N Et al.
    Cell Death Dis  2021;12:1038
  8. The integrated stress response promotes B7H6 expression.
    Authors: Ofer Et al.
    J Mol Med (Berl)  2020;98:135-148
  9. Aripiprazole Cytotoxicity Coincides with Activation of the Unfolded Protein Response in Human Hepatic Cells.
    Authors: Angela M Et al.
    J Pharmacol Exp Ther  2020;374:452-461
  10. Pharmacological induction of selective endoplasmic reticulum retention as a strategy for cancer therapy.
    Authors: Christian Et al.
    Nat Commun  2020;11:1304

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