C16, also known as GW-506033X or PKR Inhibitor. C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. GW-506033X protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress. PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. PKR inhibitor C16 binds efficiently with human microtubule affinity-regulating kinase 4.
| Catalog Number | R023730 |
| CAS Number | 608512-97-6 |
| Synonyms | 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one; 6,8-Dihydro-8-(1H-imidazol-4-ylmethylene)- 7H-pyrrolo[2,3-g]benzothiazol-7-one; GW 506033X |
| Molecular Formula | C13H8N4OS |
| Purity | 95% |
| Target | Broad Spectrum Protein Kinase Inhibitor |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| InChIKey | VFBGXTUGODTSPK-BAQGIRSFSA-N |
| Reference | </br>1:The Specific Protein Kinase R (PKR) Inhibitor C16 Protects Neonatal Hypoxia-Ischemia Brain Damages by Inhibiting Neuroinflammation in a Neonatal Rat Model. Xiao J, Tan Y, Li Y, Luo Y.Med Sci Monit. 2016 Dec 23;22:5074-5081. PMID: 28008894 Free PMC Article</br>2:PKR-inhibitor binds efficiently with human microtubule affinity-regulating kinase 4. Naz F, Shahbaaz M, Khan S, Bisetty K, Islam A, Ahmad F, Hassan MI.J Mol Graph Model. 2015 Nov;62:245-52. doi: 10.1016/j.jmgm.2015.10.009. Epub 2015 Oct 21. PMID: 26519933 </br>3:The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. Tronel C, Page G, Bodard S, Chalon S, Antier D.Neurochem Int. 2014 Jan;64:73-83. doi: 10.1016/j.neuint.2013.10.012. Epub 2013 Nov 6. PMID: 24211709 </br>4:The PKR activator, PACT, becomes a PKR inhibitor during HIV-1 replication. Clerzius G, Shaw E, Daher A, Burugu S, Gélinas JF, Ear T, Sinck L, Routy JP, Mouland AJ, Patel RC, Gatignol A.Retrovirology. 2013 Sep 11;10:96. doi: 10.1186/1742-4690-10-96. PMID: 24020926 Free PMC Article</br>5:P58(IPK), a plant ortholog of double-stranded RNA-dependent protein kinase PKR inhibitor, functions in viral pathogenesis. Bilgin DD, Liu Y, Schiff M, Dinesh-Kumar SP.Dev Cell. 2003 May;4(5):651-61. PMID: 12737801 Free Article</br>6:Two PKR inhibitor HCV proteins correlate with early but not sustained response to interferon. Gerotto M, Dal Pero F, Pontisso P, Noventa F, Gatta A, Alberti A.Gastroenterology. 2000 Dec;119(6):1649-55. PMID: 11113086 |
