2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
EGFR:0.7 μM (IC50)
In Vivo
In Vitro
In DHER-14 cells, AG 494 inhibits Cdk2 activation and EGF-dependent DNA synthesis[2]. AG-494 significantly prevents NF-kB activation in silica-stimulated cells, and also reduces NF-kB activation in H2O2-treated cells[4]. AG-494 (3-9 μM; 5-7 days) inhibits BMP9-induced ALP activity in a dose-dependent manner[5].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Gazit A, et al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991;34(6):1896-1907.
[2]. Osherov N, et al. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997;410(2-3):187-190.
[3]. Osherov N, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem. 1993 May 25;268(15):11134-42.
[4]. Liu X, Qin J, et al. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med. 2013;17(9):1160-1172.
[5]. Jihee Lee Kang, et al. SILICA-INDUCED NUCLEAR FACTOR- k B ACTIVATION: INVOLVEMENT OF REACTIVE OXYGEN SPECIES AND PROTEIN TYROSINE KINASE ACTIVATION. Journal of Toxicology and Environmental Health, Part A.
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