FSC-231 | PICK1 PDZ domain inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $240.00 |
FSC-231 (1215849-96-9) 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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
FSC-231 (1215849-96-9) 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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