Description
Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase (IC
50 = 11 nM) that was first isolated from a
Streptomyces culture filtrate. It does not inhibit protein kinase A (PKA), PKC, or PI3K (IC
50s > 100 μM). It has been used to differentiate rat mesenchymal stem cells, to inhibit NMDA-stimulated cGMP production, and to inhibit VEGF-induced angiogenesis.
Chemical Properties
Off-White Solid
Uses
A potent tyrosine kinase inhibitor. Inhibition is competitive with ATP and is noncompetitive with the peptide.
Definition
ChEBI: 5-[(2,5-dihydroxyphenyl)methyl-[(2-hydroxyphenyl)methyl]amino]-2-hydroxybenzoic acid is an aromatic amine.
Biological Activity
Potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC 50 = 11 nM). Inhibits p60 c-src with an IC 50 of 500 nM and is selective over PKA, PKC and PI 3-kinase (IC 50 > 100 μ M).
target
EGFR | PKC | PI3K | Calcium Channel
References
[1] TOSHIHIKO ONODA. Isolation of a Novel Tyrosine Kinase Inhibitor, Lavendustin A, from Streptomyces griseolavendus[J]. Journal of Natural Products , 1989, 52 6: 1252-1257. DOI:
10.1021/np50066a009[2] C Y HSU. Kinetic analysis of the inhibition of the epidermal growth factor receptor tyrosine kinase by Lavendustin-A and its analogue.[J]. The Journal of Biological Chemistry, 1991, 266 31: 21105-21112.
[3] KI-CHUL HWANG. Chemicals that modulate stem cell differentiation.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008: 7467-7471. DOI:
10.1073/pnas.0802825105[4] THOMAS J. O’’DELL Seth G N G Eric R Kandel. Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors[J]. Nature, 1991, 353 6344: 558-560. DOI:
10.1038/353558a0[5] T P FAN R B R Jaggar. Controlling the vasculature: angiogenesis, anti-angiogenesis and vascular targeting of gene therapy.[J]. Trends in pharmacological sciences, 1995, 16 2: 57-66. DOI:
10.1016/s0165-6147(00)88979-8
