Molecular Formula | C13H8N4OS |
Molar Mass | 268.29 |
Density | 1.604±0.06 g/cm3(Predicted) |
Boling Point | 674.6±55.0 °C(Predicted) |
Solubility | Soluble in DMSO |
Appearance | Orange to orange brown solid |
Color | yellow to orange-brown |
pKa | 10.20±0.20(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 2 years from date of purchsae as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Use | PKR-IN-C16 are specific protein kinase (PKR) inhibitors. PKR-IN-C16 can inhibit the autophosphorylation of PKR, and the translation blockade induced by PKR in primary neuron cell culture can be relieved by PKR-IN-C16. 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. |
Hazard Symbols | Xi - Irritant![]() |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
Reference Show more | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.727 ml | 18.637 ml | 37.273 ml |
5 mM | 0.745 ml | 3.727 ml | 7.455 ml |
10 mM | 0.373 ml | 1.864 ml | 3.727 ml |
5 mM | 0.075 ml | 0.373 ml | 0.745 ml |