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529542

Sigma-Aldrich

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

Quality Level

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
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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