508307 Grp94 Inhibitor, PU-WS13 - Calbiochem

508307
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₂₀Cl₂N₆S

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable 6-amino-purine based compound that selectively binds to Grp94 and inhibits its activity (EC50 = 220 nM). Exhibits much reduced activity towards other paralogs (EC50 = 27 µM, 42 µM, and 7.3 µM for Hsp90α, Hsp90β and Trap-1, respectively). Disrupts HER2 architecture in plasma membrane and reduces the viability of HER2 over-expressing SKBr3 breast cancer cells in a dose-dependent manner. Blocks their proliferation at the sub-G1 phase and induces apoptosis. Causes rapid inactivation of Raf-1-MAP kinase signaling at the membrane, but not in the cytosol indicating the requirement of Grp94 for HER2 architecture. Does not appear to be toxic to non-malignant cells. Unlike pan-Hsp90 and the cytosolic Hsp90 inhibitors, it does not activate any feedback heat-shock response.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number508307
      Brand Family Calbiochem®
      Synonyms8-((3,5-Dichlorophenyl)thio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine
      References
      ReferencesPatel, P.D., et al. 2013. Nat. Chem. Biol. 9,677.
      Product Information
      FormWhite powder
      Hill FormulaC₁₇H₂₀Cl₂N₆S
      Chemical formulaC₁₇H₂₀Cl₂N₆S
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGrp94
      Primary Target IC<sub>50</sub>EC₅₀ = 220 nM
      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 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Grp94 Inhibitor, PU-WS13 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Patel, P.D., et al. 2013. Nat. Chem. Biol. 9,677.
      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.

      Revision20-June-2014 JSW
      Synonyms8-((3,5-Dichlorophenyl)thio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine
      DescriptionA cell-permeable 6-amino-purine based compound that selectively binds to Grp94 and inhibits its activity (EC50 = 220 nM). Exhibits much reduced activity towards other paralogs (EC50 = 27 µM, 42 µM, and 7.3 µM for Hsp90α, Hsp90β and Trap-1, respectively). Disrupts HER2 architecture in plasma membrane and reduces the viability of HER2 over-expressing SKBr3 breast cancer cells in a dose-dependent manner. Blocks their proliferation at the sub-G1 phase and induces apoptosis. Causes rapid inactivation of Raf-1-MAP kinase signaling at the membrane, but not in the cytosol indicating the requirement of Grp94 for HER2 architecture. Does not appear to be toxic to non-malignant cells. Unlike pan-Hsp90 and the cytosolic Hsp90 inhibitors, it does not activate any feedback heat-shock response.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₂₀Cl₂N₆S
      Purity≥98% by HPLC
      SolubilityDMSO (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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesPatel, P.D., et al. 2013. Nat. Chem. Biol. 9,677.