GSK 2606414

Name: GSK 2606414
Brand: Tocris Bioscience
SKU: 5107

Tocris Bioscience, part of Bio-Techne | Catalog # 5107

Citations (58)

COA / SDS

Potent and selective PERK inhibitor; orally bioavailable

Key Product Details

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% (HPLC)
Molecular Weight:	451.44

View Full Technical Details for GSK 2606414

Technical Data
Citations

Biological Activity for GSK 2606414

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.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Compound Libraries for GSK 2606414

GSK 2606414 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2606414

M. Wt	451.44
Formula	C₂₄H₂₀F₃N₅O
Storage	Store at -20°C
Purity	≥99% (HPLC)
CAS Number	1337531-36-8
PubChem ID	53469448
InChi Key	SIXVRXARNAVBTC-UHFFFAOYSA-N
Smiles	NC1=NC=NC2=C1C(C3=CC(CCN4C(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4C=C3)=CN2C

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.

Solubility for GSK 2606414

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	45.14	100

Preparing Stock Solutions for GSK 2606414

The following data is based on the product molecular weight 451.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.22 mL	11.08 mL	22.15 mL
5 mM	0.44 mL	2.22 mL	4.43 mL
10 mM	0.22 mL	1.11 mL	2.22 mL
50 mM	0.04 mL	0.22 mL	0.44 mL

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References for GSK 2606414

References are publications that support the biological activity of the product.

Harding Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 2012 PMID: 23148209
Axten Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J.Med.Chem. 2012 PMID: 22827572