508307 Grp94 Inhibitor, PU-WS13 - Calbiochem

508307
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₂₀Cl₂N₆S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08307.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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
          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

          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.