373226 Hdm2 E3 Ligase Inhibitor II, HLI373 - CAS 502137-98-6 - Calbiochem

373226
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₂₃N₅O₂ • 2HCl 502137-98-6

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      373226-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable pyrimidoquinoline-dione compound that upregulates cellular p53 and E3 ubiquitin ligase HDM2/MDM2 protein levels (optimal conc. = 5 µM in RPE cells) by directly inhibiting MDM2 E3 ubiquitin ligase activity. Shown to induce apoptotic cell death in E1A-transformed, but not non-transformed, RPE cells and be more active toward wild-type p53-expressing than mutant p53-expressing cancer cells (≥67% vs. ≤37% death induction, respectively; 25 µM 30 h treatment).
          Catalogue Number373226
          Brand Family Calbiochem®
          SynonymsMDM2 Inhibitor VI, MDM2 E3 Ligase Inhibitor II, 5-(3-Dimethylaminopropylamino)-3,10-dimethyl-10H-pyrimido[4,5-b]quinoline-2,4-dione, 2HCl
          References
          ReferencesKitagaki, J., et al. 2008. Mol. Cancer Ther. 7, 2445.
          Yang, Y., et al. 2005. Cancer Cell 7, 547.
          Product Information
          CAS number502137-98-6
          FormCream solid
          Hill FormulaC₁₈H₂₃N₅O₂ • 2HCl
          Chemical formulaC₁₈H₂₃N₅O₂ • 2HCl
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
          Toxicity Regulatory Review
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Kitagaki, J., et al. 2008. Mol. Cancer Ther. 7, 2445.
          Yang, Y., et al. 2005. Cancer Cell 7, 547.
          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.

          Revision26-March-2012 JSW
          SynonymsMDM2 Inhibitor VI, MDM2 E3 Ligase Inhibitor II, 5-(3-Dimethylaminopropylamino)-3,10-dimethyl-10H-pyrimido[4,5-b]quinoline-2,4-dione, 2HCl
          DescriptionA cell-permeable pyrimidoquinoline-dione compound that promotes cellular p53 and E3 ubiquitin ligase HDM2/MDM2 built-ups (optimal conc. = 5 µM in human retinal pigment epithelial RPE cells) via direct inhibition of MDM2-mediated p53 ubiquitination and MDM2 autoubiquitination, resulting in an upregulation of p53-dependent transcription activity (2.5-fold of basal in U2OS-based reporter assays; 5 µM 20 h treatment). Shown to induce apoptotic cell death in E1A-transformed, but not non-transformed, RPE cells (72% death; 10 µM 26 h treatment) and be more active toward wild-type p53-expressing than mutant p53-expressing cancer cells (≥67% vs. ≤37% death induction, respectively; 25 µM 30 h treatment).
          FormCream solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number502137-98-6
          Chemical formulaC₁₈H₂₃N₅O₂ • 2HCl
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityH₂O (50 mg/ml)
          Storage +2°C to +8°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Regulatory Review
          ReferencesKitagaki, J., et al. 2008. Mol. Cancer Ther. 7, 2445.
          Yang, Y., et al. 2005. Cancer Cell 7, 547.