bs-80235C

DATASHEET

Formulation powder

Storage: RT

Product Information:

Molecular Weight:313.14

Formula:C13H10Cl2N2O3

Purity:>98%

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

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

Description:

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.1,2 Attenuates cocaine seeking in a rodent model.3 Blocks PICK1-induced anti-inflammatory effect in acute liver injury.4