PKR Inhibitor III, 7DG

Cell permeable: yes

Primary Target
PKR

Reversible: yes

Toxicity: Standard Handling (A)

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.

Hett, E.C., et al. 2013. Nat. Chem. Biol.9, 398.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany