GSK-2606414

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.

Product information

CAS Number: 1337531-36-8

Molecular Weight: 451.44

Formula: C24H20F3N5O

Synonym:

GSK 2606414

GSK2606414

GSK PERK Inhibitor

GSK-2606414

Chemical Name: 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone

Smiles: CN1C=C(C2=C(N)N=CN=C12)C1=CC=C2C(CCN2C(=O)CC2=CC(=CC=C2)C(F)(F)F)=C1

InChiKey: SIXVRXARNAVBTC-UHFFFAOYSA-N

InChi: 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)

Technical Data

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

In Vitro:

GSK-2606414 inhibits PERK activation in cells.

In Vivo:

GSK-2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.

References:

1. 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.
2. 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.
3. 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.