Biochem/physiol Actions

Primary TargetDYRK/CLK

Cell permeable: yes

General description

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.

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.

A cell permeable, 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)