506282 | PAD Inhibitor, Cl-amidine - Calbiochem

506282
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₂₀ClF₃N₄O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      506282-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable compound that acts as a pan PAD inhibitor (IC50 = 0.8 µM, 6.2 µM and 5.9 µM for PAD1, PAD3, and PAD4, respectively) in enzymatic assays. It preferentially inactivates the calcium bound form of PAD4 in an irreversible manner, and is shown to complete with BAEE for the active site residue of this enzyme. A small but significant reduction in the efficiency of p300GDB-GRIP1 interaction is observed in transiently transfected CV-1 cells treated with Cl-amidine at concentrations between 25 µM and 200 µM, in vivo . Furthermore, this compound (200 µM) together with HDAC inhibitor SAHA (0.4 µM) has shown additive effects in inducing p21, GADD45, and PUMA expression and inhibiting cancer cell growth in a p53-dependent manner in U2OS cells.
          Catalogue Number506282
          Brand Family Calbiochem®
          SynonymsN-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
          References
          ReferencesKnuckley, B., et al. 2010. Biochemistry 23, 4852.
          Li, P., et al. 2010. Oncogene 21, 3153.
          Luo, Y., et al. 2006. Biochemistry 39, 11727.
          Product Information
          FormWhite solid
          Hill FormulaC₁₆H₂₀ClF₃N₄O₄
          Chemical formulaC₁₆H₂₀ClF₃N₄O₄
          Structure formula ImageStructure formula Image
          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 with Blue Ice or with Dry Ice
          Toxicity Regulatory Review
          Storage -20°C
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          506282

          References

          Reference overview
          Knuckley, B., et al. 2010. Biochemistry 23, 4852.
          Li, P., et al. 2010. Oncogene 21, 3153.
          Luo, Y., et al. 2006. Biochemistry 39, 11727.
          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.

          Revision04-November-2011 RFH
          SynonymsN-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
          DescriptionA cell-permeable compound that acts as a pan PAD inhibitor (IC50 = 0.8 µM, 6.2 µM and 5.9 µM for PAD1, PAD3, and PAD4, respectively) in enzymatic assays. It preferentially inactivates the calcium bound form of PAD4 in an irreversible manner, and is shown to complete with BAEE for the active site residue of this enzyme. A small but significant reduction in the efficiency of p300GDB-GRIP1 interaction is observed in transiently transfected CV-1 cells treated with Cl-amidine at concentrations between 25 µM and 200 µM, in vivo. Furthermore, this compound (200 µM) together with HDAC inhibitor SAHA (0.4 µM) has shown additive effects in inducing p21, GADD45, and PUMA expression and inhibiting cancer cell growth in a p53-dependent manner in U2OS cells.
          FormWhite solid
          Chemical formulaC₁₆H₂₀ClF₃N₄O₄
          Structure formulaStructure formula
          Purity>95% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          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 Regulatory Review
          ReferencesKnuckley, B., et al. 2010. Biochemistry 23, 4852.
          Li, P., et al. 2010. Oncogene 21, 3153.
          Luo, Y., et al. 2006. Biochemistry 39, 11727.