553513 Rac Inhibitor III, EHop-016 - CAS 1380432-32-5 - Calbiochem

553513
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₅H₃₀N₆O 1380432-32-5

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      553513-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable NSC23766 (Cat. No. 553502) analog that is more selective against Rac interaction with Vav2 (by 45% blockage at 4 µM) than Tiam (35% blockage at 50 µM) and ~100-times more potent than NSC23766 in suppressing Rac1-GTP level in MDA-MB-435 (IC50 = 1.1 vs. 95 µM, respectively) cultures. Effectively inhibits PAK Thr423 phosphorylation (IC50 <2 µM), while reducing Cdc42-GTP level only at higher concentrations (by 18% at 5 µM), in MDA-MB-435 cultures.
          Catalogue Number553513
          Brand Family Calbiochem®
          SynonymsN⁴-(9-Ethyl-9H-carbazol-3-yl)-N²-(3-morpholin-4-yl-propyl)-pyrimidine-2,4-diamine
          References
          ReferencesMontalvo-Ortiz, B.L., et al. 2012. J. Biol. Chem. 287, 13228.
          Product Information
          CAS number1380432-32-5
          FormPale yellow powder
          Hill FormulaC₂₅H₃₀N₆O
          Chemical formulaC₂₅H₃₀N₆O
          Structure formula ImageStructure formula Image
          Applications
          ApplicationRac Inhibitor III, EHop-016, CAS 1380432-32-5, is a cell-permeable analog of NSC23766. It is ~100-fold more potent than NSC23766 in suppressing Rac1-GTP level in MDA-MB-435 cells.
          Biological Information
          Purity≥96% 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 Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          Rac Inhibitor III, EHop-016 - CAS 1380432-32-5 - Calbiochem Certificates of Analysis

          TitleLot Number
          553513

          References

          Reference overview
          Montalvo-Ortiz, B.L., et al. 2012. J. Biol. Chem. 287, 13228.
          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.

          Revision20-September-2013 JSW
          SynonymsN⁴-(9-Ethyl-9H-carbazol-3-yl)-N²-(3-morpholin-4-yl-propyl)-pyrimidine-2,4-diamine
          DescriptionA cell-permeable carbazolylpyrimidine compound that inhibits Rac GEF interaction (by 45% of Vav2 interaction at 4 µM and by 35% of Tiam1 DH/PH domain interaction at 50 µM) by directly targeting Rac GEF binding domain and effectively reduces cellular Rac1-GTP (IC50 = 1.1 and 3 µM, respectively, in MDA-MB-435 and MDA-MB-231 cells) and Rac3-GTP (IC50 <1 µM in MDA-MB-435 cells) as well as PAK Thr423 phosphorylation (by 55% and 84%, respectively, at 2 and 4 µM in MDA-MB-435 cells), suppressing MDA-MB-435 Cdc42-GTP level only at higher concentrations (by 5%, 18% and 75%, respectively, at 4, 5, and 10 µM) and enhancing, instead of downregulating, RhoA-GTP level, presumably due to a cellular compensatory mechanism in response to Rac inhibition. NSC23766 (Cat. No. 553502), in comparison, is much less potent in reducing Rac1-GTP level in MDA-MB-435 (IC50 = 95 µM), but 10-times more effective in disrupting Rac1 and Tiam-1 DH/PH domain interaction.
          FormPale yellow powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1380432-32-5
          Chemical formulaC₂₅H₃₀N₆O
          Structure formulaStructure formula
          Purity≥96% by HPLC
          SolubilityDMSO (50 mg/ml; clear, pale yellow solution)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesMontalvo-Ortiz, B.L., et al. 2012. J. Biol. Chem. 287, 13228.