Inhibiteur de domaine PICK1 PDZ; FSC231

Non disponible en dehors du Royaume-Uni et de l'Irlande

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 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.

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Regulatory Review (Z)