658403

AG 538

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM).

• Sinônimo(s): AG 538, α-Cyano-(3,4-dihydroxy)cinnamoyl-(3ʹ,4ʹ-dihydroxyphenyl)ketone, Tyrphostin AG 538
• Fórmula empírica (Notação de Hill): C₁₆HN₁₁O₅
• Número CAS: 133550-18-2
• Peso molecular: 427.25
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: dark orange to brown
• solubilidade: DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM). Reaction is competitive with respect to IGF-1R substrate. Also inhibits the phosphorylation of PTK substrate poly(Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC₅₀ = 60 nM, 113 nM, 370 nM, and 2.4 µM, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC₅₀ = 76 µM).

A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1R (insulin-like growth factor-1 receptor) kinase autophosphorylation (IC₅₀ = 400 nM). Also inhibits the phosphorylation of PTK substrate poly (Glu,Tyr) by IGF-1R, IR, EGF-R, and Src (IC₅₀ = 60 nM, 113 nM, and 2.4 µM respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC₅₀ = 76 µM). Inhibition is competitive with respect to the substrate binding site of IGF-1R kinase. Also inhibits the authophosphorylation of IGF-1R and the activation of PKB and ERK₂ in NIH-3T3 cells over-expressing IGF-1R.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
IGF-1 receptor kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 400 nM against IGF-1 receptor kinase

Embalagem

Packaged under inert gas

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

Blum, G., et al. 2000. Biochemistry39, 15705.

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