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.

• 别名: Postsynaptic Density Protein-95 Inhibitor, Tat-N-dimer
• 分類程式碼代碼: 12352200

属性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: solid
• 效力: 4.6 nM K_i
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 100 mg/mL; water: 100 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C

说明

一般說明

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.

生化／生理作用

Cell permeable: yes

Primary Target
PSD95

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外觀

Supplied as a trifluoroacetate salt.

重構

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

其他說明

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

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 1
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable