For research use only. Not for therapeutic Use.
PKR inhibitors(Cat No.: R023730) are compounds that block the activity of protein kinase R (PKR), an enzyme involved in the cellular response to stress, particularly viral infections. PKR is activated by double-stranded RNA and plays a key role in initiating antiviral immune responses, but its overactivation can contribute to inflammation and diseases such as neurodegeneration and cancer. PKR inhibitors are being investigated for therapeutic potential in treating viral infections, autoimmune diseases, and certain cancers by modulating immune responses and reducing unwanted inflammation.
| 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 | Apoptosis |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | (8Z)-8-(1H-imidazol-5-ylmethylidene)-6H-pyrrolo[2,3-g][1,3]benzothiazol-7-one |
| InChI | 1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3- |
| InChIKey | VFBGXTUGODTSPK-BAQGIRSFSA-N |
| SMILES | C1=CC2=C(C\3=C1NC(=O)/C3=C\C4=CN=CN4)SC=N2 |
| 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 |
