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530266 Cytohesin Inhibitor II, Cyplecksin 2 - Calbiochem

Selectively and covalently modifies the pleckstrin homology domain of the cytohesin family (Kd ~ 2 µM to cytohesin-1) and irreversibly inhibits its function.

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Synonyme: 5-Benzyl-5-bromo-1-(4-chlorophenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, Cytohesin pleckstrin homology domain inhibitor 2, Cyth PH Domain Inhibitor

Primary Target: pleckstrin homology domain of the cytohesin family
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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₇H₁₂BrClN₂O₃
      Description
      Overview

      This product has been discontinued.



      A cell-permeable 5-bromobarbiturate that selectively and covalently modifies the pleckstrin homology (PH) domain of the cytohesin family (Kd ~ 2 µM to cytohesin-1 labeled with Alexa647) and irreversibly inhibits its function. Prevents the interaction cytohesin-1 PH, and to cytohesins 1 and 2 lacking the short C-terminal polybasic region with PIP3 and PIP2. Blocks insulin-dependent cytohesin-2-GFP translocation to plasma membrane in HeLa cells (~50 µM). Does not recognize or show any binding to T-lymphoma invasive and metastasis inducing protein 1 (Tiam)-DH-PH and shows poor affinity towards Sec7 domain of cytohesin-2. Cytohesins Inhibitor SecinH3 is also available (Cat. No. 565725).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530266
      Brand Family Calbiochem®
      Synonyms5-Benzyl-5-bromo-1-(4-chlorophenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, Cytohesin pleckstrin homology domain inhibitor 2, Cyth PH Domain Inhibitor
      References
      ReferencesHussein, M., et al. 2013. Angew. Chem. Int. Ed., 52, 9529.
      Product Information
      FormWhite solid
      Hill FormulaC₁₇H₁₂BrClN₂O₃
      Chemical formulaC₁₇H₁₂BrClN₂O₃
      ReversibleN
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetpleckstrin homology domain of the cytohesin family
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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 Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Protect from Moisture Protect from moisture
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      530266 0

      Documentation

      Cytohesin Inhibitor II, Cyplecksin 2 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Hussein, M., et al. 2013. Angew. Chem. Int. Ed., 52, 9529.
      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.

      Revision27-June-2014 JSW
      Synonyms5-Benzyl-5-bromo-1-(4-chlorophenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, Cytohesin pleckstrin homology domain inhibitor 2, Cyth PH Domain Inhibitor
      DescriptionA cell-permeable 5-bromobarbiturate that targets the PH domain of cytohesin family small GEFs (Kd ~2 µM in binding assay using Cyth1 PH domain aa259-381) via covalent interaction and effectively competes against both PIP2 and PIP3 for Cyth PH domain binding (IC50 ≤10 µM against 30 nM PIP2; [Cyth1 PH] = 250 nM), while exhibiting no affinity toward Tiam1 DH-PH domain and displaying little potency against GEP100-PH/PIP2, DAGK- PH/PIP2, ARHGAP25-PH/PIP3, IRS1-PH/PIP2, Pleckstrin-PH/PIP3, or Akt2/PIP3 interaction even at concentrations as high as 100 µM. Overnight pretreatment (50 µM) prior to insulin stimulation (100 nM for 10 min) is shown to greatly inhibit insulin-induced Cyth2 plasma membrane translocation by 83% in HeLa Cyth2-GFP transfectants. Greatly complements the Sec7 domain-targeting SecinH3 (Cat. No. 565725) in studying Cytohesins-mediated cellular signaling events.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₂BrClN₂O₃
      Purity≥97% by HPLC
      SolubilityEthanol (50 mg/ml)
      Storage Protect from moisture
      Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Toxicity Standard Handling
      ReferencesHussein, M., et al. 2013. Angew. Chem. Int. Ed., 52, 9529.