Synonym
GW-506033X; GW 506033X; GW506033X; C16, PKR Inhibitor; PKR-IN-C16; Protein Kinase RNA-activated
IUPAC/Chemical Name
6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one
InChi Key
VFBGXTUGODTSPK-BAQGIRSFSA-N
InChi Code
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-
SMILES Code
O=C1/C(C2=C(SC=N3)C3=CC=C2N1)=C\C4=CN=CN4
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).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
268.29
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
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.
0951.jpg "C16 (PKR Inhibitor)")
