Bulk Inquiry
GSK 2606414
Axon 2233
CAS:
1337531-36-8
Purity:
99%
- Soluble in DMSO
- MF: C24H20F3N5O
- MW: 451.44
Description
Potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK or EIF2AK3) with IC50 value of 0.4 nM and >1000 fold selectivity over EIF2AK1 (HRI) and EIF2AK2 (PKR). Overall, good selectivity was observed, with only 20 protein kinases inhibited >85% by GSK 2606414 at 10 μM during screening against a panel of 294 kinases. It inhibits the growth of a human tumor xenograft in mice with good oral bioavailability and blood-brain barrier penetration.PERK is a type I ER membrane protein and one of three primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis.
More Information
| Parent CAS No. | 1337531-36-8 |
|---|---|
| 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 | C1C=C2N(C(=O)CC3C=C(C(F)(F)F)C=CC=3)CCC2=CC=1C1=CN(C)C2N=CN=C(N)C1=2 |
| MFCD | N.A. |
| 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) |
| InChiKey | SIXVRXARNAVBTC-UHFFFAOYSA-N |
| CID | 53469448 |
| Short Description | PERK inhibitor |
References
- J.M. Axten et al. 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 PERK (...). J. Med. Chem. 2012, 55, 7193-7207.
- J.A. Moreno et al. Oral Treatment Targeting the Unfolded Protein Response Prevents Neurodegeneration and Clinical Disease in Prion-Infected Mice. Science Translational Medicine 2013, 5(206), 206ra138.
- List of publications using GSK 2606414 (Axon 2233) purchased from Axon Medchem
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1542 | NVP-AUY922 |
From $82.50 |
| 1543 | CNF 2024 |
From $88.00 |
| 1608 | VER 155008 |
From $104.50 |
| 1856 | PU-H71 trihydrochloride |
From $115.50 |
| 1968 | STA 9090 |
From $115.50 |
| 2251 | Apoptozole |
From $104.50 |
| 2278 | ISRIB |
From $104.50 |
| 2567 | Azoramide |
From $71.50 |
| 2720 | A-92 |
From $154.00 |
| 4249 | Salubrinal |
From $121.00 |
Other Categories
Get a Quote for
Loading...