504540 EBP1 Inhibitor, WS6 - Calbiochem

504540
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₉H₃₁F₃N₆O₃ • xHCl

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      Glass bottle 10 mg
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      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®
      SynonymsErb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor, N-(6-(4-(2-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylamino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide, xHCl
      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
      Quality LevelMQ100
      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

      EBP1 Inhibitor, WS6 - Calbiochem 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
      SynonymsErb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor, N-(6-(4-(2-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylamino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide, xHCl
      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.