Description
Tyrphostin 9 (10537-47-0) inhibits PDGF receptor tyrosine kinase (IC50?= 1.2 μM)1and is a potent (10 nM) inhibitor of oxidative phosphorylation2. Inhibits cell growth by disrupting mitochondria.3 Tyrphostin 9 perturbs the golgi complex and blocks proliferation of vascular smooth muscle cells.4
Uses
Tyrphostin A9 can be used for inhibiting tyrosine kinase functions in C2C12 cells. It has also been used to disrupt membrane potential in mammalian cells.
Uses
Selective inhibitor of PDGF receptor tyrosine kinase
Uses
SF 6847 is an inhibitor of EGFR with IC50 of 460 μM.
Definition
ChEBI: Malonoben is an alkylbenzene. It has a role as a geroprotector.
Production Methods
Commercial synthesis details for malonoben are not available in open literature but its structure and classification allow its manufacturing process to be inferred from standard industrial practice. Based on its identity its commercial manufacture would have relied on assembling a hindered phenolic precursor (a 3,5 di tert butyl 4 hydroxybenzaldehyde derivative) followed by Knoevenagel type condensation with malononitrile to form the characteristic benzylidene malononitrile scaffold. This type of condensation is widely used in industrial production of substituted malononitriles and requires controlled basic or acidic catalysis to maintain selectivity and prevent side reactions. Final purification, typically crystallisation, would yield technical grade malonoben for formulation.
General Description
A selective, cell-permeable, reversible, and substrate competitive inhibitor of the platelet-derived growth factor receptor tyrosine kinase (IC50 = 500 nM). Anti-proliferative agent. Uncoupler of oxidative phosphorylation. Induces apoptosis in vitro and cell growth arrest in NHL cell lines.
Biological Activity
Potent uncoupler of oxidative phosphorylation.
Biochem/physiol Actions
Cell permeable: yes
Mechanism of action
Uncouples respiratory phosphorylation. Stomach and contact action
References
1) Bilder?et al. (1991),?Tyrphostins inhibit PDGF-induced DNA synthesis and associated early events in smooth muscle cells; Am. J. Physiol.,?260?C721
2) Terada?et al. (1981),?The interaction of highly active uncouplers with mitochondria; Biochim. Biophys. Acta,?639?225
3) Burger?et al. (1995),?Tyrphostin AG17, [3,5-Ditert-butyl-4-hydroxybenzylidene)-malononitrile], inhibits cell growth by disrupting mitochondria; Cancer Res.,?55?2794
4) Thyberg?et al. (1998),?Tyrphostin A9 and wortmannin perturb the Golgi complex and block proliferation of vascular smooth muscle cells; Eur. J. Cell Biol.,?76?33
Pesticide Type
Insecticide; Acaricide
