GSK 2606414 | Tocris Bioscience 5107/10 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

GSK 2606414

catalog :

5107/10

quantity :

10 mg (also 50 mg)

price :

349 USD

more info or order :

Tocris Bioscience product webpage

citations: 16

Reference
Jeong H, Hong E, Ahn J, Cho J, Jeong J, Kim C, et al. ERdj5 protects goblet cells from endoplasmic reticulum stress-mediated apoptosis under inflammatory conditions. Exp Mol Med. 2023;55:401-412 pubmed publisher
Saaoud F, Liu L, Xu K, Cueto R, Shao Y, Lu Y, et al. Aorta- and liver-generated TMAO enhances trained immunity for increased inflammation via ER stress/mitochondrial ROS/glycolysis pathways. JCI Insight. 2023;8: pubmed publisher
Khoonkari M, Liang D, Lima M, van der Land T, Liang Y, Sun J, et al. The Unfolded Protein Response Sensor PERK Mediates Stiffness-Dependent Adaptation in Glioblastoma Cells. Int J Mol Sci. 2022;23: pubmed publisher
Huis In t Veld L, Ho N, Wassink M, den Brok M, Adema G. Saponin-based adjuvant-induced dendritic cell cross-presentation is dependent on PERK activation. Cell Mol Life Sci. 2022;79:231 pubmed publisher
Zaepfel B, Rothstein J. Polyadenylated RNA and RNA-Binding Proteins Exhibit Unique Response to Hyperosmotic Stress. Front Cell Dev Biol. 2021;9:809859 pubmed publisher
Sheshadri N, Poria D, Sharan S, Hu Y, Yan C, Koparde V, et al. PERK signaling through C/EBPδ contributes to ER stress-induced expression of immunomodulatory and tumor promoting chemokines by cancer cells. Cell Death Dis. 2021;12:1038 pubmed publisher
Nabar N, Heijjer C, Shi C, Hwang I, Ganesan S, Karlsson M, et al. LRRK2 is required for CD38-mediated NAADP-Ca2+ signaling and the downstream activation of TFEB (transcription factor EB) in immune cells. Autophagy. 2021;:1-19 pubmed publisher
. Aripiprazole Cytotoxicity Coincides with Activation of the Unfolded Protein Response in Human Hepatic Cells. J Pharmacol Exp Ther. 2020;374:452-461 pubmed publisher
Mahameed M, Boukeileh S, Obiedat A, Darawshi O, Dipta P, Rimon A, et al. Pharmacological induction of selective endoplasmic reticulum retention as a strategy for cancer therapy. Nat Commun. 2020;11:1304 pubmed publisher
Obiedat A, Charpak Amikam Y, Tai Schmiedel J, Seidel E, Mahameed M, Avril T, et al. The integrated stress response promotes B7H6 expression. J Mol Med (Berl). 2020;98:135-148 pubmed publisher
Samluk L, Urbanska M, Kisielewska K, Mohanraj K, Kim M, Machnicka K, et al. Cytosolic translational responses differ under conditions of severe short-term and long-term mitochondrial stress. Mol Biol Cell. 2019;:mbcE18100628 pubmed publisher
Mahameed M, Wilhelm T, Darawshi O, Obiedat A, Tommy W, Chintha C, et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis. 2019;10:300 pubmed publisher
Piccolis M, Bond L, Kampmann M, Pulimeno P, Chitraju C, Jayson C, et al. Probing the Global Cellular Responses to Lipotoxicity Caused by Saturated Fatty Acids. Mol Cell. 2019;74:32-44.e8 pubmed publisher
Park S, Lim Y, Lee D, Elvira R, Lee J, Lee M, et al. Modulation of Protein Synthesis by eIF2α Phosphorylation Protects Cell from Heat Stress-Mediated Apoptosis. Cells. 2018;7: pubmed publisher
Leznicki P, Natarajan J, Bader G, Spevak W, Schlattl A, Abdul Rehman S, et al. Expansion of DUB functionality generated by alternative isoforms - USP35, a case study. J Cell Sci. 2018;131: pubmed publisher
Topf U, Suppanz I, Samluk L, Wrobel L, Böser A, Sakowska P, et al. Quantitative proteomics identifies redox switches for global translation modulation by mitochondrially produced reactive oxygen species. Nat Commun. 2018;9:324 pubmed publisher

product information

brand :

Tocris, a Bio-Techne Brand

catalog number base :

5107

SKU :

5107/10

product name :

GSK 2606414

Description :

Potent and selective PERK inhibitor; orally bioavailable

target :

PERK Inhibitors

category :

Small Molecules

unit size :

10 mg (also 50 mg)

purity :

99%

observed molecular weight :

451.44

url print :

?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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.

extended description :

Potent and selective PERK inhibitor; orally bioavailable

chemical name text :

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

formula :

C 24 H 20 F 3 N 5 O

formula text :

C24H20F3N5O

cas num :

1337531-36-8

USD :

349 USD

product details :

Potent and selective PERK inhibitor; orally bioavailable

storage :

Store at -20°C

more info or order :

Tocris Bioscience product webpage