Date published: 2026-5-7

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AGL 2263

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Application:
AGL 2263 is a cell-permeable benzoxazolone-containing bioisostere of tyrphostin AG 538; acts as an inhibitor of insulin receptor
Molecular Weight:
322.28
Molecular Formula:
C17H10N2O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AGL 2263 is a cell-permeable benzoxazolone-containing bioisostere of tyrphostin AG 538 that acts as a potent, substrate-competitive, but not ATP-competitive, inhibitor of IR (insulin receptor) and IGF-IR (insulin-like growth factor-1 receptor). AGL 2263 is selective towards IR and IGF-IR (IC50 = 0.4 and 0.43 muM, respectively) and inhibits c-Src (Src) and Akt (PKB) at much higher concentrations (IC50 = 2.2 and 55 muM, respectively) in kinase assays. AGL 2263 may act to prevent IGF-1-induced cellular IGF-IR autophosphorylation and down stream signalling. Specifically inhibits IGF-1-induced, but not PDGF-induced, activation of Akt (PKB) in cells. AGL 2263 effectively blocks the formation of colonies in soft agar by breast and prostate cancer cells. Exhibits improved cellular oxidative stability than AG 538.


AGL 2263 References

  1. 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
  2. Formation of E-cadherin-mediated cell-cell adhesion activates AKT and mitogen activated protein kinase via phosphatidylinositol 3 kinase and ligand-independent activation of epidermal growth factor receptor in ovarian cancer cells.  |  Reddy, P., et al. 2005. Mol Endocrinol. 19: 2564-78. PMID: 15928314
  3. Vanadium and insulin increase adiponectin production in 3T3-L1 adipocytes.  |  Seale, AP., et al. 2006. Pharmacol Res. 54: 30-8. PMID: 16524741
  4. Molecular mechanism of bis(maltolato)oxovanadium(IV)-induced insulin signaling in 3T3-L1 and IM9 cells: impact of dexamethasone.  |  Bose, S., et al. 2007. J Mol Endocrinol. 38: 627-49. PMID: 17556533
  5. Visfatin causes endothelium-dependent relaxation in isolated blood vessels.  |  Yamawaki, H., et al. 2009. Biochem Biophys Res Commun. 383: 503-8. PMID: 19393628
  6. Multi-pathway cellular analysis of compound selectivity.  |  Hancock, MK., et al. 2010. Mol Biosyst. 6: 1834-43. PMID: 20593073
  7. Somatic cells initiate primordial follicle activation and govern the development of dormant oocytes in mice.  |  Zhang, H., et al. 2014. Curr Biol. 24: 2501-8. PMID: 25438940
  8. JAK3 inhibitor VI is a mutant specific inhibitor for epidermal growth factor receptor with the gatekeeper mutation T790M.  |  Nishiya, N., et al. 2015. World J Biol Chem. 6: 409-18. PMID: 26629323
  9. Procyanidin B1 and p-Coumaric Acid from Highland Barley Grain Showed Synergistic Effect on Modulating Glucose Metabolism via IRS-1/PI3K/Akt Pathway.  |  Liu, ZH. and Li, B. 2021. Mol Nutr Food Res. 65: e2100454. PMID: 34342938
  10. Chlorogenic acid and β-glucan from highland barley grain ameliorate β-cell dysfunction via inhibiting apoptosis and improving cell proliferation.  |  Liu, ZH. and Li, B. 2021. Food Funct. 12: 10040-10052. PMID: 34515712

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AGL 2263, 5 mg

sc-221223
5 mg
$357.00