530266 Cytohesin Inhibitor II, Cyplecksin 2 - Calbiochem

530266
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₂BrClN₂O₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30266.0001
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          Glass bottle 10 mg
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          Description
          OverviewA 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
          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

          Documentation

          Cytohesin Inhibitor II, Cyplecksin 2 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Hussein, M., et al. 2013. Angew. Chem. Int. Ed., 52, 9529.
          Data Sheet

          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 -20°C
          Protect from moisture
          Protect from light
          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.