5.32089

Dual DYRK/CLK inhibitor, Cpd 23

• Synonyme(s) : Dual DYRK/CLK inhibitor, Cpd 23, Pre-mRNA Splicing Modulator, DYRK Inhibitor, Cdc2-like Kinase Inhibitor
• Formule empirique (notation de Hill): C₁₀H₈O₂S
• Numéro CAS: 56363-81-6
• Poids moléculaire : 192.23
• Numéro MDL: MFCD24717135
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥95% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 60 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: −20°C
• Chaîne SMILES: O=C(C)C1=CC2=CC(O)=CC=C2S1

Description

Description générale

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).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
DYRK/CLK

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable