HDBA, a derivative of a Streptomyces griseolavendus butyl acetate extract, is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with an IC50 value of 0.012 µM.1 HDBA also inhibits pp60c-src(+) kinase and Ca2+ calmodulin-dependent kinase II with IC50 values of 0.5 and 0.2 µM, respectively.2 At a concentration of 10-150 µM, HDBA inhibits tyrosine kinase-associated neutrophil degranulation and superoxide generation.3
1
Onoda, T., Iinuma, H., Sasaki, Y., et al. Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J Nat Prod52(6)1252-1257(1989).
2
O'Dell, T.J., Kandel, E.R., and Grant, S.G.N. Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors. Nature353558-560(1991).
3
Burt, H.M., Jackson, J.K., and Salari, H. Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor. J Leukoc Biol55112-119(1994).
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SMILES
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Oc1ccc(O)c(CNc2ccc(O)c(c2)C(=O)O)c1
Background Reading
Onoda, T., Iinuma, H., Sasaki, Y., et al. Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus. J Nat Prod52(6)1252-1257(1989).
Burt, H.M., Jackson, J.K., and Salari, H. Inhibition of crystal-induced neutrophil activation by a protein tyrosine kinase inhibitor. J Leukoc Biol55112-119(1994).
O'Dell, T.J., Kandel, E.R., and Grant, S.G.N. Long-term potentiation in the hippocampus is blocked by tyrosine kinase inhibitors. Nature353558-560(1991).
Lavendustin C is available in the following screening
library: