529531

PICK1 PDZ Domain Inhibitor, FSC231

The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications.

• Synonym(s): PICK1 PDZ Domain Inhibitor, FSC231, ( E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate, (E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
• Empirical Formula (Hill Notation): C₁₃H₁₀Cl₂N₂O₃
• Molecular Weight: 313.14
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not PDZ domains of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (K_i ~10 µM in competitive binding assays), GluR2 (K_i ~10 µM in competitive binding assays), and mRluR7a (~70% inhibition by Co-IP using lysates from 50 µM FSC231-treated HEK293), c-terminus binding to PICK1 PDZ. Shown to accelerate GluR2 surface recycling after NMDR-induced internalization (t_1/2 = 7.5 vs 10 min with and without 50 µM FSC231 treatment) in rat hippocampal neurons and prevent both LTD (% long-term depression = 74 vs 50 with and without 50 µM FSC231 treatment) and LTP (% long-term potentiation = 137 vs 266 with and without 50 µM FSC231 treatment) in murine hippocampal slices.

A cell-permeable acryloylcarbamate compound that selectively targets the PDZ (PSD-95/Discs-large/ZO-1 homology) domain of PICK1 (protein interacting with C kinase 1), but not those of PSD-95 (postsynaptic density protein 95) and GRIP1 (glutamate receptor interacting protein 1), effectively competing against dopamine transporter/DAT (K_i ~10 µM), GluR2 (K_i ~10 µM), and mRluR7a, c-terminus binding to PICK1 PDZ. Shown to accelerate internalized GluR2 surface recycling and suppress both long-term depression and potentiation in rat and murine hippocampal neurons.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconsitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Thorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA107, 413.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable