Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. The c-ErbB-specific tyrphostin AG30 specifically blocked STAT5 activation, implicating this signal transducer in c-ErbB-induced self renewal[1]. Treatment of human colon cancer cell lines, LS 174T, COLO 205, and SW620, with sodium butyrate and 8-Cl-cAMP or tyrphostins AG-30 and AG-34, significantly attenuated TPK (tyrosine protein kinase) activity concomitantly with an increase in the activity of alkaline phosphatase, an enzymatic marker of intestinal cell differentiation. The induction of the differentiated phenotype in colon cancer cells is associated with a marked decrease in TPK activity and tyrosine phosphorylation[2]. Preincubation of B lymphocytes with two different tyrphostins blocked anti-IgM-induced tyrosine phosphorylation and actin polymerization[3].
Tyrphostin AG30 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human aortic endothelial cells (HAEC)
0.1, 1.0, 10 μg/ml
1, 2, 4 days
To evaluate the effect of AG-30 on endothelial cell growth, results showed AG-30 increased MTS activity in a dose-dependent manner and was more potent than LL-37.
J Cell Mol Med. 2009 Mar;13(3):535-46
Human aortic smooth muscle cells (HASMC)
0.1, 1.0, 10 μg/ml
1, 3, 5 days
To evaluate the effect of AG-30 on smooth muscle cell growth, results showed AG-30 increased MTS activity in a dose-dependent manner.
J Cell Mol Med. 2009 Mar;13(3):535-46
Human aortic endothelial cells (HAEC)
10 μg/ml
24 hours
To evaluate the effect of AG-30 on endothelial cell migration, results showed AG-30 significantly increased cell migration.
J Cell Mol Med. 2009 Mar;13(3):535-46
RBL-2H3 cells
0.1 – 1.5 µM
30 minutes
AG-30/5C induces dose-dependent degranulation in RBL-2H3 cells stably expressing MRGPRX2, but native RBL-2H3 cells do not respond to AG-30/5C.
J Immunol. 2019 Feb 15;202(4):1229-1238
LAD2 cells
0.01 – 1.5 µM
30 minutes
AG-30/5C induces degranulation in LAD2 cells via MRGPRX2 with an EC50 value of <0.1 μM and maximal response at 1.0 −1.5 μM.
J Immunol. 2019 Feb 15;202(4):1229-1238
Human aortic endothelial cells (HAEC)
0.1, 1.0, 10 μg/ml
4 hours
To evaluate the chemotactic migration effect of AG-30 on endothelial cells, results showed AG-30 had chemotactic action.
J Cell Mol Med. 2009 Mar;13(3):535-46
Human umbilical vein endothelial cells (HUVECs)
10 μg/ml
48 hours
Evaluate the effect of AG30/5C on HUVECs proliferation, results showed AG30/5C significantly increased HUVECs proliferation.
PLoS One. 2014 Mar 27;9(3):e92597
Human aortic endothelial cells (HAEC)
0.1, 1.0, 10 μg/ml
7 days
To evaluate the effect of AG-30 on endothelial tube formation, results showed AG-30 promoted tube formation more effectively than LL-37 or control peptide.
J Cell Mol Med. 2009 Mar;13(3):535-46
Human epidermal keratinocytes cell line (HaCaT cells)
0, 0.1, 1, and 10 μg/ml
Second day
AG30/5C induced cell growth of HaCaT cells in a dose-dependent manner.
J Cell Mol Med. 2012 Jul;16(7):1629-39
Tyrphostin AG30 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 male mice
Ischemic hind limb model
Intramuscular injection
100 μg, 500 μg
Single injection, lasted for 28 days
To evaluate the angiogenic effect of AG-30 in ischemic hind limb model, results showed AG-30 significantly increased blood flow and capillary density.
J Cell Mol Med. 2009 Mar;13(3):535-46
Mice
Diabetic mouse wound-healing model
Topical application
100 μg/ml
Repeated on days 0, 2, 4, 7, 9, 11, 14, and 16 after operation
The topical application of AG30/5C accelerated wound healing with increased angiogenesis and attenuated MRSA infection.
J Cell Mol Med. 2012 Jul;16(7):1629-39
SKHAV transgenic mice
ΛsupFG1 shuttle-reporter transgenic mice
Intradermal injection
50μg
Injections on days 1 and 3, tissue harvested 10 days after the last treatment
In hairless mice, AG30 introduced gene modifications in both tail and back skin via intradermal delivery, with mutation frequencies 4-fold higher than PBS controls.
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