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).
生化/生理作用
Cell permeable: yes
Primary Target DYRK/CLK
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Schmitt, C., et al. 2014. ACS Med. Chem. Lett.5, 963.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany