220488 Chk2 Inhibitor, PV1019 - Calbiochem

220488
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      Přehled

      Replacement Information

      Tabulka spec. kláve

      Empirical Formula
      C₁₈H₁₇N₇O₃

      Ceny a dostupnost

      Katalogové číslo DostupnostBalení ks/bal. Cena Množství
      220488-10MG
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      Dostupné omezené množství
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          Skleněná láhev 10 mg
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          Vyžádat nacenění
          Description
          OverviewA cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50 = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50 = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50 <10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/- cultures.
          Catalogue Number220488
          Brand Family Calbiochem®
          SynonymsNSC 744039
          References
          ReferencesJobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.
          Product Information
          FormOrange solid
          Hill FormulaC₁₈H₁₇N₇O₃
          Chemical formulaC₁₈H₁₇N₇O₃
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliqout 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

          Chk2 Inhibitor, PV1019 - Calbiochem MSDS

          Title

          Safety Data Sheet (SDS) 

          Chk2 Inhibitor, PV1019 - Calbiochem Certificates of Analysis

          TitleLot Number
          220488

          References

          Přehled odkazů
          Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.
          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.

          Revision30-August-2010 RFH
          SynonymsNSC 744039
          DescriptionA cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50 = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50 = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50 <10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/- cultures.
          FormOrange solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₈H₁₇N₇O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (5 mg/ml)
          Storage -20°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesJobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.