Molecular structure of AG 538, CAS Number: 133550-18-2
AG 538 (CAS 133550-18-2)
See product citations (4)
Alternate Names:
α-Cyano-(3,4-dihydroxy)cinnamoyl-(3′,4′-dihydroxyphenyl)ketone
Application:
AG 538 is A potent, competitive inhibitor of IGF-1 receptor kinase
CAS Number:
133550-18-2
Purity:
≥95%
Molecular Weight:
297.3
Molecular Formula:
C16H1NO5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
AG 538 is a potent, competitive inhibitor of IGF-IR (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 muM, respectively). Inhibits the phosphorylation of PKB at a much higher concentration (IC50 = 76 muM).
AG 538 (CAS 133550-18-2) References
- Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimics. | Blum, G., et al. 2003. J Biol Chem. 278: 40442-54. PMID: 12869569
- Receptor tyrosine kinase and phosphoinositide-3 kinase signaling in malignant mesothelioma. | Rascoe, PA., et al. 2005. J Thorac Cardiovasc Surg. 130: 393-400. PMID: 16077404
- Aberrant NF-kappaB activity in HaCaT cells alters their response to UVB signaling. | Lewis, DA., et al. 2006. J Invest Dermatol. 126: 1885-92. PMID: 16741515
- Stromelysin-3 over-expression enhances tumourigenesis in MCF-7 and MDA-MB-231 breast cancer cell lines: involvement of the IGF-1 signalling pathway. | Kasper, G., et al. 2007. BMC Cancer. 7: 12. PMID: 17233884
- Role of insulin-like growth factor-1R system in colorectal carcinogenesis. | Donovan, EA. and Kummar, S. 2008. Crit Rev Oncol Hematol. 66: 91-8. PMID: 17977741
- Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1. | Simeonov, A., et al. 2009. PLoS One. 4: e5740. PMID: 19484131
- δ-Opioid receptors stimulate GLUT1-mediated glucose uptake through Src- and IGF-1 receptor-dependent activation of PI3-kinase signalling in CHO cells. | Olianas, MC., et al. 2011. Br J Pharmacol. 163: 624-37. PMID: 21250979
- Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays. | Mukherjee, S., et al. 2012. Nucleic Acids Res. 40: 8607-21. PMID: 22740655
- Hepatitis C virus NS3 inhibitors: current and future perspectives. | Salam, KA. and Akimitsu, N. 2013. Biomed Res Int. 2013: 467869. PMID: 24282816
- Phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ), a lipid signalling enigma. | Giudici, ML., et al. 2016. Adv Biol Regul. 61: 47-50. PMID: 26710750
- Insulin-like growth factor (IGF)-II- mediated fibrosis in pathogenic lung conditions. | Garrett, SM., et al. 2019. PLoS One. 14: e0225422. PMID: 31765403
- DHEA inhibits proliferation, migration and alters mesenchymal-epithelial transition proteins through the PI3K/Akt pathway in MDA-MB-231 cells. | Colín-Val, Z., et al. 2021. J Steroid Biochem Mol Biol. 208: 105818. PMID: 33508440
- Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrophostins: potent inhibitors of EGF receptor tyrosine kinase in vitro. | Gazit, A., et al. 1996. J Med Chem. 39: 4905-11. PMID: 8960549
Inhibitor of:
IGF-IR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
AG 538, 5 mg | sc-203807 | 5 mg | $153.00 |