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509454 WNK Signaling Inhibitor, Compound B - Calbiochem

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.