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509454 WNK Signaling Inhibitor, Compound B - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 7-Ethoxy-3-N-(furan-2-ylmethyl)acridine-3,9-diamine, SPAK/OSR1 Inhibitor, STE20/SPS1-Related Proline-Alanine Rich Protein Kinase Inhibitor, Oxidative Stress-Responsive Kinase-1 Inhibitor

Primary Target: CCT (conserved c-terminal) domain of SPAK and OSR1
509454
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₀H₁₉N₃O₂
      Description
      Overview

      This product has been discontinued.



      A cell-permeable diaminoacridine derivative that targets the CCT domain of SPAK and OSR1 via reversible binding (Kd = 20 µM; rat SPAK-CCT452-553 GST fusion) and thereby prevents CCT-mediated interaction of SPAK/OSR1 with RFXV/I motif-containing binding partners, including upstream kinases WNK1/4 and downstream substrates NCC/NKCC. Shown to selectively suppress hypotonic shock-induced WNK signaling pathway activation in mpkDCT and MOVAS (100 µM) cultures without affecting p38 MAPK phosphorylation.
      Catalogue Number509454
      Brand Family Calbiochem®
      Synonyms7-Ethoxy-3-N-(furan-2-ylmethyl)acridine-3,9-diamine, SPAK/OSR1 Inhibitor, STE20/SPS1-Related Proline-Alanine Rich Protein Kinase Inhibitor, Oxidative Stress-Responsive Kinase-1 Inhibitor
      References
      ReferencesMori, T., et al. 2013. Biochem. J. 455, 339.
      Product Information
      FormBright yellow powder
      Hill FormulaC₂₀H₁₉N₃O₂
      Chemical formulaC₂₀H₁₉N₃O₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCCT (conserved c-terminal) domain of SPAK and OSR1
      Primary Target K<sub>i</sub>20 µ
      Purity≥97% 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 +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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      509454 0

      Documentation

      WNK Signaling Inhibitor, Compound B - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Mori, T., et al. 2013. Biochem. J. 455, 339.
      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.

      Revision21-February-2014 JSW
      Synonyms7-Ethoxy-3-N-(furan-2-ylmethyl)acridine-3,9-diamine, SPAK/OSR1 Inhibitor, STE20/SPS1-Related Proline-Alanine Rich Protein Kinase Inhibitor, Oxidative Stress-Responsive Kinase-1 Inhibitor
      DescriptionA cell-permeable diaminoacridine derivative that targets the CCT (conserved c-terminal) domain of SPAK and OSR1 via reversible affinity binding (Kd = 20 µM in binding studies using recombinant rat SPAK-CCT452-553 GST fusion) and thereby prevents CCT-mediated interaction of SPAK/OSR1 with RFXV/I motif-containing binding partners, including upstream kinases WNK1/4 (With no-lysine kinases 1 & 4) and downstream substrates NCC/NKCC (Na+-Cl- co-transporter & Na+-K+-2Cl- co-transporter). Shown to selectively suppress hypotonic shock-induced WNK signaling pathway activation in mpkDCT (69% and 51% inhibition of NCC and SPAK phosphorylation, respectively at 100 µM) and MOVAS (70% and 77% inhibition of NKCC and SPAK phosphorylation, respectively at 100 µM) cultures without affecting p38 MAPK phosphorylation.
      FormBright yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₉N₃O₂
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesMori, T., et al. 2013. Biochem. J. 455, 339.