All Photos(1)
Synonym(s):
PKR Inhibitor III, 7DG, Double-stranded RNA-activated Protein Kinase Inhibitor III, EIF2AK2 Inhibitor III, 7-Desacetoxy-6,7-dehydrogedunin, Double-stranded RNA-dependent Protein Kinase Inhibitor III, Double-stranded RNA-dependent Protein Kinase Inhibitor III, Double-stranded RNA-activated Protein Kinase Inhibitor III, EIF2AK2 Inhibitor III, 7-Desacetoxy-6,7-dehydrogedunin
Empirical Formula (Hill Notation):
C26H30O5
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Assay
≥95% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 25 mg/mL
storage temp.
2-8°C
General description
A cell-permeable gedunin analog that directly targets PKR via reversible interaction inhibits PKR-mediated cellular events by disrupting PKR signaling complexes assembly, such as IκK complex and inflammasome/pyroptosome, resulting in effective blockage of LPS-induced IκBβ degradaion (20 µM) and protection against anthrax toxin LT-induced caspase-1 activation as well as subsequent pyroptosis (10 µM) in murine macrophage J774 cultures. PKR is also known to mediate LT-induced apoptosis via its kinase activity in LPS-primed Macrophages derived from C57BL/6 with a resistent NLRP1 allele, inhibitable by C16 (Cat. Nos. 527450 & 527451), but not by 7DG, while LT-induced pyroptosis in J774 cultures is insensitive to C16 treatment.
A cell-permeable gedunin analog that directly targets PKR via reversible interaction without competing against ATP binding and inhibits PKR-mediated cellular events by disrupting PKR signaling complex assembly, such as IκK complex and inflammasome/pyroptosome, resulting in effective blockage of LPS-induced IκBβ degradaion (20 µM 7DG added 2 h prior to 10 ng/mL LPS) and protection against anthrax toxin LT-induced caspase-1 activation as well as subsequent pyroptosis (by 50% and 100%, respectively, at 5 and 10 µM; 2 h 7DG pretreatment prior to 6 h LT incubation) in J774A.1 BALB/c-derived murine macrophage J774 cultures. PKR is also known to mediate LT-induced apoptosis via its kinase activity in LPS-primed Macrophages derived from C57BL/6 with a resistent NLRP1 allele, inhibitable by C16 (Cat. Nos. 527450 & 527451), but not by 7DG, while LT-induced pyroptosis in J774 cultures is inhibited by 7DG, but insensitive to C16 treatment.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKR
PKR
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Other Notes
Hett, E.C., et al. 2013. Nat. Chem. Biol.9, 398.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Signal Word
Warning
Hazard Statements
Precautionary Statements
Hazard Classifications
Acute Tox. 4 Oral
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
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