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.

• 別名: Postsynaptic Density Protein-95 Inhibitor, Tat-N-dimer
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• 有効性: 4.6 nM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL; water: 100 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
PSD95

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

物理的形状

Supplied as a trifluoroacetate salt.

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable