220488 Chk2 Inhibitor, PV1019 - Calbiochem

220488
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₇N₇O₃

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220488-10MG
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      Glass bottle 10 mg
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      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 SDS

      Title

      Safety Data Sheet (SDS) 

      Chk2 Inhibitor, PV1019 - Calbiochem Certificates of Analysis

      TitleLot Number
      220488

      References

      Reference overview
      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.