529542
PSD95 Inhibitor, Tat-N-dimer
The PSD95 Inhibitor, Tat-N-dimer controls the biological activity of PSD95. This small molecule/inhibitor is primarily used for Cancer applications.
Synonym(s):
Postsynaptic Density Protein-95 Inhibitor, Tat-N-dimer
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About This Item
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
solid
potency
4.6 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL, water: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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 (Ki = 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 t1/2 ~ 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PSD95
PSD95
Reversible: yes
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Bach, A., et al. 2012. Proc Natl Acad Sci USA.109 3317.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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