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504540 EBP1 Inhibitor, WS6 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₉H₃₁F₃N₆O₃ • xHCl

Products

Catalog NumberPackaging Qty/Pack
5.04540.0001 Glass bottle 10 mg
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
Global Trade Item Number
Catalog Number GTIN
5.04540.0001 04055977244885

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 Protect from light
-20°C
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.
Toxicity Standard Handling
ReferencesShen, W., et al. 2013. J. Am. Chem. Soc. 135, 1669.