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The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications.
More>>The PICK1 PDZ Domain Inhibitor, FSC231 controls the biological activity of PICK1. This small molecule/inhibitor is primarily used for Neuroscience applications. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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 (Ki ~10 µM), GluR2 (Ki ~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.
Thorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA107, 413.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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 (Ki ~10 µM in competitive binding assays), GluR2 (Ki ~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 (t1/2 = 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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₁₃H₁₀Cl₂N₂O₃
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconsitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Regulatory Review
References
Thorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA107, 413.
