658403
AG 538
A potent, cell-premeable, reversible, and competitive inhibitor of IGF-1 receptor kinase (IC₅₀ = 400 nM).
Synonym(s):
AG 538, α-Cyano-(3,4-dihydroxy)cinnamoyl-(3ʹ,4ʹ-dihydroxyphenyl)ketone, Tyrphostin AG 538
Sign Into View Organizational & Contract Pricing
All Photos(1)
About This Item
Empirical Formula (Hill Notation):
C16HN11O5
CAS Number:
Molecular Weight:
427.25
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
dark orange to brown
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IGF-1 receptor kinase
IGF-1 receptor kinase
Product competes with ATP.
Reversible: yes
Target IC50: 400 nM against IGF-1 receptor kinase
Packaging
Packaged under inert gas
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
Blum, G., et al. 2000. Biochemistry39, 15705.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service