504540 | EBP1 Inhibitor, WS6 - Calbiochem

504540
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
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₉H₃₁F₃N₆O₃ • xHCl

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04540.0001
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          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 phenoxypyrimidin-cyclopropanecarboxamide compound that effectively stimulates the growth of primary β cells in cultured primary rat and human islets in vitro (ECmax in 4 d = 200 and 400 nM, respectively) and in the murine type 1 diabetes (T1D) model RIP-DTA in vivo (170% of control pancreas Ki-67-positive β cells in 1 wk; 5 mg/kg i.p. q.o.d.) by interacting with IKKε and EBP1/PA2G4/Erb3 binding protein-1 and blocking the known suppressor function of EBP1 toward E2F-mediated transcription. Likewise, dual inhibition of EBP1 (with shRNA) and IKK (1 µM; Cat. Nos. 401486 & 505378) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells.
          Catalogue Number504540
          Brand Family Calbiochem®
          SynonymsN-(6-(4-(2-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylamino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide, xHCl, Erb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor
          References
          ReferencesShen, W., et al. 2013. J. Am. Chem. Soc. 135, 1669.
          Product Information
          FormWhite powder
          Hill FormulaC₂₉H₃₁F₃N₆O₃ • xHCl
          Chemical formulaC₂₉H₃₁F₃N₆O₃ • xHCl
          Hygroscopic Hygroscopic
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetEBP1/PA2G4/Erb3 binding protein-1
          Secondary targetIKKε
          Purity≥98% 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 -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Shen, W., et al. 2013. J. Am. Chem. Soc. 135, 1669.
          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.

          Revision18-December-2013 JSW
          SynonymsN-(6-(4-(2-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylamino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide, xHCl, Erb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor
          DescriptionA cell-permeable phenoxypyrimidin-cyclopropanecarboxamide compound that effectively stimulates the growth of primary β cells in cultures in vitro (ECmax in 4 d = 200 and 400 nM, respectively, for increasing Ki-67-positive β cell population in primary rat and human islets) and in the murine type 1 diabetes (T1D) model RIP-DTA in vivo (170% of control pancreas Ki-67-positive β cells in 1 wk and 150% of control pancreas β cell mass in 6 wks; 5 mg/kg i.p. q.o.d.) with significant blood glucose reducing efficacy (200 vs. 425 mg/dL on d45 with or without treatment). WS6 is shown to interact with IKKε and EBP1/PA2G4/Erb3 binding protein-1 as well as upregulate cellular E2F mRNA (2.8- and 4.8-fold of vehicle control, respectively, with 8 h and 12 h treatment; 1 µM) and transcription activity (1.4- and 1.5-fold of vehicle control, respectively, at 0.74 and 2.22 µM; 24 h treatment) in murine β cell line R7T1, consistent with blocking the known suppressor function of EBP1 toward E2F-mediated transcription. Likewise, dual inhibition of EBP1 (with shRNA) and IKK (1 µM; Cat. Nos. 401486 & 505378) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₉H₃₁F₃N₆O₃ • xHCl
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml) or H₂O (100 mg/ml)
          Storage -20°C
          Hygroscopic
          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
          ReferencesShen, W., et al. 2013. J. Am. Chem. Soc. 135, 1669.