GSK 2606414
Tocris Bioscience, part of Bio-Techne | Catalog # 5107
Potent and selective PERK inhibitor; orally bioavailable
Key Product Details
Description
Potent and selective PERK inhibitor; orally bioavailable
Product Description
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 GlaxoSmithKlineProduct Specifications
Molecular Weight
451.44
Formula
C24H20F3N5O
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for GSK 2606414
For research use only
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