5.32089

Dual DYRK/CLK inhibitor, Cpd 23

• Synonym(s): Dual DYRK/CLK inhibitor, Cpd 23, Pre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
• Empirical Formula (Hill Notation): C₁₀H₈O₂S
• CAS Number: 56363-81-6
• Molecular Weight: 192.23
• MDL number: MFCD24717135
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• potency: 60 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 50 mg/mL
• storage temp.: −20°C
• SMILES string: O=C(C)C1=CC2=CC(O)=CC=C2S1

Description

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.

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, 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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
DYRK/CLK

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable