5.32089

Dual DYRK/CLK inhibitor, Cpd 23

• Sinônimo(s): Dual DYRK/CLK inhibitor, Cpd 23, Pre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
• Fórmula empírica (Notação de Hill): C₁₀H₈O₂S
• Número CAS: 56363-81-6
• Peso molecular: 192.23
• Número MDL: MFCD24717135
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥95% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• potência: 60 nM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: O=C(C)C1=CC2=CC(O)=CC=C2S1

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
DYRK/CLK

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable