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529531 PICK1 PDZ Domain Inhibitor, FSC231 - Calbiochem

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

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Synonyme: (E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate

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529531
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

Empirical Formula
C₁₃H₁₀Cl₂N₂O₃

Preis & Verfügbarkeit

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529531-10MG
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      Description
      OverviewA 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.
      Catalogue Number529531
      Brand Family Calbiochem®
      Synonyms(E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
      References
      ReferencesThorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 413.
      Product Information
      FormOff-white solid
      Hill FormulaC₁₃H₁₀Cl₂N₂O₃
      Chemical formulaC₁₃H₁₀Cl₂N₂O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconsitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      529531-10MG 04055977269697

      Documentation

      PICK1 PDZ Domain Inhibitor, FSC231 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      PICK1 PDZ Domain Inhibitor, FSC231 - Calbiochem Analysenzertifikate

      TitelChargennummer
      529531

      Literatur

      Übersicht
      Thorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 413.
      Datenblatt

      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.

      Revision22-March-2012 JSW
      Synonyms(E)-Ethyl-2-cyano-3-(3,4-dichlorophenyl)acryloylcarbamate
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₃H₁₀Cl₂N₂O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconsitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesThorsen, T.S., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 413.