GSK-2606414 is an orally available, potent, and selective PERK inhibitor. GSK2606414 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.
Chemical Formula: C24H20F3N5O
Exact Mass: 451.16199
Molecular Weight: 451.44
Elemental Analysis: C, 63.85; H, 4.47; F, 12.63; N, 15.51; O, 3.54
GSK PERK Inhibitor
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Jiang X, Wei Y, Zhang T, Zhang Z, Qiu S, Zhou X, Zhang S. Effects of GSK2606414 on cell proliferation and endoplasmic reticulum stress associated gene expression in retinal pigment epithelial cells. Mol Med Rep. 2017 May;15(5):3105-3110. doi: 10.3892/mmr.2017.6418. Epub 2017 Mar 30. PubMed PMID: 28358434.
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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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