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Product Details

FSC-231 | PICK1 PDZ domain inhibitor

FSC-231 is 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

References/Citations

1) Thorsen et al. (2010), Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD; Proc. Natl. Acad. Sci. USA, 107 413
2) Tang et al. (2013), Willed-movement training reduces motor deficits and induces a PICK1-dependent LTD in rats subjected to focal cerebral ischemia; Behav. Brain Res., 256 481
3) Schmidt et al. (2013), Stimulation of mGluR5 in the accumbens shell promotes cocaine seeking by activating PKC gamma; J. Neuroscience, 33 14160
4) Xie et al. (2016), PICK1 confers anti-inflammatory effects in acute liver injury via suppressing M1 macrophage polarization; Biochemie, 127 121

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Focus Biomolecules cell signaling supplier, chemical structure of FSC-231 | PICK1 PDZ domain inhibitor | CAS 1215849-96-9

Catalog#  10-1406-0005

$60.00
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Catalog Number:
10-1406
Activity:
PICK1 PDZ domain inhibitor
Chemical Name:
(E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
Molecular Weight:
313.14
Molecular Formula:
C13H10Cl2N2O3
Solubility:
Soluble in DMSO (up to 35 mg/ml with warming) or in Ethanol (up to 18 mg/ml with warming)
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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