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573110 STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem

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Synonymes: 1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one

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573110
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Tableau de caractéristiques principal

CAS #Empirical Formula
2062-78-4C₂₈H₂₉F₂N₃O

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573110-100MG
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      Description
      Overview

      This product has been discontinued.



      A cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D1, D2, D3, D4, α1-/α2-adrenergic, and 5-HT2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction.
      Catalogue Number573110
      Brand Family Calbiochem®
      Synonyms1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one
      References
      ReferencesChen, J., et al. 2011. Chem. Biol 18, 1390.
      Nelson, E.A., et al. 2011. Blood 117, 3421.
      Product Information
      CAS number2062-78-4
      FormWhite solid
      Hill FormulaC₂₈H₂₉F₂N₃O
      Chemical formulaC₂₈H₂₉F₂N₃O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Ambient Temperature Only
      Toxicity Regulatory Review
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions ar 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
      Référence GTIN
      573110-100MG 04055977265965

      Documentation

      STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      573110

      Références bibliographiques

      Aperçu de la référence bibliographique
      Chen, J., et al. 2011. Chem. Biol 18, 1390.
      Nelson, E.A., et al. 2011. Blood 117, 3421.

      Informations techniques

      Titre
      JAK/STAT Signaling Research Focus
      Fiche technique

      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.

      Revision28-November-2011 JSW
      Synonyms1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one
      DescriptionA cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D1, D2, D3, D4, α1-/α2-adrenergic, and 5-HT2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction. Acts as a selective and non-competitive inhibitor of human USP1/UAF1 and USP7 activities (IC50 = 2 and 47 µM, respectively) with no effect on UCH-L1 and UCH-L3 (IC50 > 500 µM).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number2062-78-4
      Chemical formulaC₂₈H₂₉F₂N₃O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions ar stable for up to 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesChen, J., et al. 2011. Chem. Biol 18, 1390.
      Nelson, E.A., et al. 2011. Blood 117, 3421.