REST INHIBITOR X5050 1PC X 25MG (C15-1304-368)

General description

A cell-permeable benzoimidazole derivative that acts as an inhibitor of repressor element-1 silencing transcription factor (REST, a Kruppel-type zinc finger transcription factor). Induces a dose-dependent reduction in the 122 kDa isoforms of REST in HEK cells. It is believed to target REST degradation, but not its expression or binding to repressor element binding sequence. Shown to rescue REST-regulated gene expressions, such as BDNF in the prefrontal cortex in mice with quinolinic acid-induced striatal lesions. Acute ventricular delivery of X5050 increases the expression of BDNFand other REST-regulated genes. Also shown to promote the expression of BDNF and SNAP25 in human neural stem cells via degradation of REST.

A cell-permeable benzoimidazole derivative that acts as an inhibitor of repressor element-1 silencing transcription factor (REST, a Kruppel-type zinc finger transcription factor). Induces a dose-dependent reduction in the 122 kDa isoforms of REST in HEK cells. It is believed to target REST degradation, but not its expression or binding to repressor element binding sequence. Shown to rescue REST-regulated gene expressions, such as BDNF in the prefrontal cortex in mice with quinolinic acid-induced striatal lesions. Acute ventricular delivery of X5050 increases the expression of BDNFand other REST-regulated genes. Also shown to promote the expression of BDNF and SNAP25 in human neural stem cells via degradation of REST.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
REST

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Charbord, J., et al, 2013, Stem Cells31, 1816.

Legal Information

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

Molecular Weight: 309.32. Empirical Formula: C₁₇H₁₅N₃O₃. Assay: ≥. 97% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: light beige. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.