Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

532089 Dual DYRK/CLK inhibitor, Cpd 23 - Calbiochem

532089
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₀H₈O₂S
Description
Overview

This product has been discontinued.



A cell permeable 5-hydroxybenzothiophenylethanone that acts as a dual inhibitor of Cdc2-like kinase 1 (Clk1; IC50 = 60 nM) and dual specificity tyrosine phosphorylation-regulated kinases 1A/1B (Dyrk1A/1B; IC50 = 200 and 100 nM, respectively). Also inhibits Clk4 with high potency. Exhibits much reduced inhibitory effect on Haspin ( IC50 = 800 nM) and has much reduced inhibitory effect on other kinases even at higher concentration (~ 5 µM). Causes a complete disappearance of incomplete and alternatively spliced transcripts and is shown to enhance the generation of the mature Clk1 mRNA splicing product (EC50 = 8.9 µM) in cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Catalogue Number532089
Brand Family Calbiochem®
SynonymsPre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
References
ReferencesSchmitt, C., et al. 2014. ACS Med. Chem. Lett. 5, 963.
Product Information
FormYellow powder
Hill FormulaC₁₀H₈O₂S
Chemical formulaC₁₀H₈O₂S
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetDYRK/CLK
Primary Target IC<sub>50</sub>60 nM, EC₅₀
Purity≥95% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°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 3 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
532089 0

Documentation

Dual DYRK/CLK inhibitor, Cpd 23 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Schmitt, C., et al. 2014. ACS Med. Chem. Lett. 5, 963.

Technical Info

Title
Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System
White Paper: Further considerations of antibody validation and usage.
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.

Revision15-March-2015 JSW
SynonymsPre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
DescriptionA cell permeable 5-hydroxybenzothiophenylethanone that acts as a dual inhibitor of Cdc2-like kinase 1 (Clk1; IC50 = 60 nM) and dual specificity tyrosine phosphorylation-regulated kinases 1A/1B (Dyrk1A/1B; IC50 = 200 and 100 nM, respectively). Also inhibits Clk4 with high potency. Exhibits much reduced inhibitory effect on Haspin ( IC50 = 800 nM) and has much reduced inhibitory effect on other kinases even at higher concentration (~ 5 µM). Causes a complete disappearance of incomplete and alternatively spliced transcripts and is shown to enhance the generation of the mature Clk1 mRNA splicing product (EC50 = 8.9 µM) in cells.
FormYellow powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₀H₈O₂S
Purity≥95% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesSchmitt, C., et al. 2014. ACS Med. Chem. Lett. 5, 963.