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528106 PI 3-Kγ Inhibitor - CAS 648450-29-7 - Calbiochem

528106
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₁₂H₇N₃O₂S 648450-29-7

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528106-5MG
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      Description
      OverviewA cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
      Catalogue Number528106
      Brand Family Calbiochem®
      Synonyms5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
      References
      ReferencesBarber, D.F., et al. 2005. Nat. Med. 11, 933.
      Camps, M., et al. 2005. Nat. Med. 11, 936.
      Product Information
      CAS number648450-29-7
      ATP CompetitiveY
      FormPink solid
      Hill FormulaC₁₂H₇N₃O₂S
      Chemical formulaC₁₂H₇N₃O₂S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPhosphatidylinositol 3-kinase γ (PI 3-Kγ)
      Primary Target IC<sub>50</sub>8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively; 181 nM in selectively blocking MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human mono
      Primary Target K<sub>i</sub>7.8 nM
      Purity≥90% by HPLC
      Physicochemical Information
      Cell permeableY
      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 +2°C to +8°C
      Protect from Light 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.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PI 3-Kγ Inhibitor - CAS 648450-29-7 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PI 3-Kγ Inhibitor - CAS 648450-29-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      528106

      References

      Reference overview
      Barber, D.F., et al. 2005. Nat. Med. 11, 933.
      Camps, M., et al. 2005. Nat. Med. 11, 936.
      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.

      Revision14-September-2007 JSW
      Synonyms5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione, PI 3-K Inhibitor I
      DescriptionA cell-permeable, potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC50 = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.
      FormPink solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number648450-29-7
      Chemical formulaC₁₂H₇N₃O₂S
      Structure formulaStructure formula
      Purity≥90% by HPLC
      SolubilityDMSO (2.5 mg/ml)
      Storage +2°C to +8°C
      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 Standard Handling
      ReferencesBarber, D.F., et al. 2005. Nat. Med. 11, 933.
      Camps, M., et al. 2005. Nat. Med. 11, 936.