506282 PAD Inhibitor, Cl-amidine - Calbiochem

506282
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₂₀ClF₃N₄O₄

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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
      Quality LevelMQ200
      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

      PAD Inhibitor, Cl-amidine - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PAD Inhibitor, Cl-amidine - Calbiochem 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.