C16 (PKR Inhibitor)
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.
1: Naz F, Shahbaaz M, Khan S, Bisetty K, Islam A, Ahmad F, Hassan MI. PKR-inhibitor binds efficiently with human microtubule affinity-regulating kinase 4. J Mol Graph Model. 2015 Nov;62:245-52. doi: 10.1016/j.jmgm.2015.10.009. PubMed PMID: 26519933.
2: Tronel C, Page G, Bodard S, Chalon S, Antier D. The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. Neurochem Int. 2014 Jan;64:73-83. doi: 10.1016/j.neuint.2013.10.012. PubMed PMID: 24211709.
3: Clerzius G, Shaw E, Daher A, Burugu S, Gélinas JF, Ear T, Sinck L, Routy JP, Mouland AJ, Patel RC, Gatignol A. The PKR activator, PACT, becomes a PKR inhibitor during HIV-1 replication. Retrovirology. 2013 Sep 11;10:96. doi: 10.1186/1742-4690-10-96. PubMed PMID: 24020926; PubMed Central PMCID: PMC3848765.
4: Bilgin DD, Liu Y, Schiff M, Dinesh-Kumar SP. P58(IPK), a plant ortholog of double-stranded RNA-dependent protein kinase PKR inhibitor, functions in viral pathogenesis. Dev Cell. 2003 May;4(5):651-61. PubMed PMID: 12737801.
5: Gerotto M, Dal Pero F, Pontisso P, Noventa F, Gatta A, Alberti A. Two PKR inhibitor HCV proteins correlate with early but not sustained response to interferon. Gastroenterology. 2000 Dec;119(6):1649-55. PubMed PMID: 11113086.
2: Tronel C, Page G, Bodard S, Chalon S, Antier D. The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component. Neurochem Int. 2014 Jan;64:73-83. doi: 10.1016/j.neuint.2013.10.012. PubMed PMID: 24211709.
3: Clerzius G, Shaw E, Daher A, Burugu S, Gélinas JF, Ear T, Sinck L, Routy JP, Mouland AJ, Patel RC, Gatignol A. The PKR activator, PACT, becomes a PKR inhibitor during HIV-1 replication. Retrovirology. 2013 Sep 11;10:96. doi: 10.1186/1742-4690-10-96. PubMed PMID: 24020926; PubMed Central PMCID: PMC3848765.
4: Bilgin DD, Liu Y, Schiff M, Dinesh-Kumar SP. P58(IPK), a plant ortholog of double-stranded RNA-dependent protein kinase PKR inhibitor, functions in viral pathogenesis. Dev Cell. 2003 May;4(5):651-61. PubMed PMID: 12737801.
5: Gerotto M, Dal Pero F, Pontisso P, Noventa F, Gatta A, Alberti A. Two PKR inhibitor HCV proteins correlate with early but not sustained response to interferon. Gastroenterology. 2000 Dec;119(6):1649-55. PubMed PMID: 11113086.
| Chemical | |
|---|---|
| CAS Num | 608512-97-6 |
| Chemical Formula | C13H8N4OS |
| Molecular Weight | 268.294 |
| IUPAC Chemical Name | 6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one |
| Exact Mass | 268.0419 |
| Elemental Analysis | C, 58.20; H, 3.01; N, 20.88; O, 5.96; S, 11.95 |
| Synonym | GW-506033X; GW 506033X; GW506033X; C16, PKR Inhibitor. |
| Solubility | Soluble in DMSO |
| SMILES Code | O=C1/C(C2=C(SC=N3)C3=CC=C2N1)=C\C4=CN=CN4 |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >95% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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