FSC-231, PICK1 PDZ domain inhibitor

Product Details

Formal Name: (E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate

Molecular Formula: C₁₃H₁₀Cl₂N₂O₃

Formula Weight: 313.14

CAS Number: N/A

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 35 mg/ml with warming) or in Ethanol (up to 18 mg/ml with warming)

Storage: RT

Stability: ≥ 1 year.

Applications

PICK1 PDZ domain inhibitor

Functions

The first small-molecule inhibitor of the PDZ domain in protein interacting with C kinase 1 (PICK1). Binds to PICK1 PDZ domain with affinity similar to that of the endogenous peptide ligands (Ki~10.1 µM). Does not bind to PDZ domains of postsynaptic density protein 95 (PSD-95) nor glutamate receptor interacting protein 1 (GRIP1).  Pretreatment of cultured hippocampal neurons inhibits coimmunoprecipitation of the AMPA receptor GluR2 subunit with PICK1. FSC231 accelerated recycling of fluorophore-tagged GluR2 in hippocampal neurons after internalization in response to NMDA receptor activation. Blocks the expression of both long-term depression and long-term potentiation. Attenuates cocaine seeking in a rodent model. Blocks PICK1-induced anti-inflammatory effect in acute liver injury.

Application Procedures

First dissolved in DMSO (up to 35 mg/ml with warming) or in Ethanol (up to 18 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)