GSK-2606414 is an orally available, potent, and selective PERK inhibitor. GSK-2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small molecule inhibitors.
CAS Number: 1337531-36-8
Molecular Weight: 451.44
GSK PERK Inhibitor
Chemical Name: 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 90 mg/mL(199.36 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GSK-2606414 inhibits PERK activation in cells.
GSK-2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.
- Rojas-Rivera D, Delvaeye T, Roelandt R, Nerinckx W, Augustyns K, Vandenabeele P, Bertrand MJM. When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157. Cell Death Differ. 2017 Apr 28. doi: 10.1038/cdd.2017.58. [Epub ahead of print] PubMed PMID: 28452996.
- Wen L, Xiao B, Shi Y, Han F. PERK signalling pathway mediates single prolonged stress-induced dysfunction of medial prefrontal cortex neurons. Apoptosis. 2017 Jun;22(6):753-768. doi: 10.1007/s10495-017-1371-5. PubMed PMID: 28391375.
- Sharma R, Quilty F, Gilmer JF, Long A, Byrne AM. Unconjugated secondary bile acids activate the unfolded protein response and induce golgi fragmentation via a src-kinase-dependant mechanism. Oncotarget. 2017 Jan 3;8(1):967-978. doi: 10.18632/oncotarget.13514. PubMed PMID: 27888615; PubMed Central PMCID: PMC5352210.
Products are for research use only. Not for human use.
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