PSD95 Inhibitor, Tat-N-dimer

A cell-permeable, dimeric pentapeptide (IETDV) derived from GluN2B C-terminal and linked through a polyethylene glycol (PEG)-based linker that inhibits the ternary protein complex of PSD-95 (postsynaptic density protein-95), nNOS, and NMDA by directly binding to the tandem PDZ1 and 2 domains of PSD-95 (K_i = 4.6 nM). This inhibition results in the uncoupling between NMDA receptor activity and nitric oxide production without affecting NMDA-mediated ion channel gating function and pro-survival signaling pathways. Exhibits about 1000-fold higher potency than the monomeric Tat-NR2B9c. Exhibits improved plasma stability, with t_1/2 ~ 80 hours. Shown to cross the blood-brain barrier and reduce infarct volume by about 40% and restore motor functions in mice subjected to focal ischemic brain damage.

Cell permeable: yes

Primary Target
PSD95

Reversible: yes

Packaged under inert gas

Supplied as a trifluoroacetate salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Bach, A., et al. 2012. Proc Natl Acad Sci USA.109 3317.

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

Toxicity: Standard Handling (A)