AG 538-CAS 133550-18-2-Calbiochem

C₁₆HN₁₁O₅

427.25

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.

Cell permeable: yes
Primary Target
IGF-1 receptor kinase
Target IC₅₀: 400 nM against IGF-1 receptor kinase
Product competes with ATP.
Reversible: yes

Toxicity: Standard Handling (A)

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

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

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

dark orange to brown

DMSO: 5 mg/mL

ambient

−20℃

5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3