10537-47-0 Usage
Description
Tyrphostin A9 is a selective, cell-permeable, reversible, and substrate competitive inhibitor of the platelet-derived growth factor receptor tyrosine kinase. It is a potent inhibitor of oxidative phosphorylation and has anti-proliferative properties. Tyrphostin A9 can induce apoptosis in vitro and cell growth arrest in NHL cell lines. It also perturbs the Golgi complex and blocks proliferation of vascular smooth muscle cells.
Uses
Used in Pharmaceutical Industry:
Tyrphostin A9 is used as an inhibitor of tyrosine kinase functions in C2C12 cells for studying the role of tyrosine kinases in cell signaling and proliferation.
Used in Cancer Research:
Tyrphostin A9 is used as a selective inhibitor of PDGF receptor tyrosine kinase for investigating its role in cancer cell proliferation and as a potential therapeutic agent against various types of cancer.
Used in Cell Biology Research:
Tyrphostin A9 is used as an uncoupler of oxidative phosphorylation to study the effects of mitochondrial dysfunction on cell growth and apoptosis.
Used in Membrane Potential Disruption:
Tyrphostin A9 is used to disrupt membrane potential in mammalian cells for research purposes, particularly in understanding the role of membrane potential in cellular processes.
Biological Activity
Potent uncoupler of oxidative phosphorylation.
Biochem/physiol Actions
Cell permeable: yes
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
Check Digit Verification of cas no
The CAS Registry Mumber 10537-47-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 1,0,5,3 and 7 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 10537-47:
(7*1)+(6*0)+(5*5)+(4*3)+(3*7)+(2*4)+(1*7)=80
80 % 10 = 0
So 10537-47-0 is a valid CAS Registry Number.
InChI:InChI=1/C18H22N2O/c1-17(2,3)14-8-12(7-13(10-19)11-20)9-15(16(14)21)18(4,5)6/h7-9,21H,1-6H3
10537-47-0Relevant articles and documents
METHODS AND COMPOSITIONS FOR TREATING OBESITY, PREVENTING WEIGHT GAIN, PROMOTING WEIGHT LOSS, PROMOTING SLIMMING, OR TREATING OR PREVENTING THE DEVELOPMENT OF DIABETES
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Page/Page column 40; 41, (2016/01/25)
The present invention relates to compositions and kits including a chemical uncoupler, such as tyrphostin 9 or precursor or a salt thereof, and compositions including a chemical uncoupler, such as tyrphostin 9 in combination with one or more therapeutic agents, for example, L-carnitine, which are useful, for example, in treating obesity, preventing weight gain, promoting weight loss/slimming, and/or treating or preventing the development of diabetes.
Tyrphostins I: Synthesis and Biological Activity of Protein Tyrosine Kinase Inhibitors
Gazit, Aviv,Yaish, Pnina,Gilon, Chaim,Levitzki, Alexander
, p. 2344 - 2352 (2007/10/02)
A novel class of low molecular weight proteine kinase inhibitors is described.These compounds consitute a systematic series of molecules with a progressive increase in affinity toward the substrate site of the EGF receptor kinase domain.These competitive inhibitors also effectively block the EGF-dependent autophosphorylation of the receptor.The potent EGF receptor kinase blockers examined were found to competitively inhibit the homologous insulin receptor kinase at 102-103 higher inhibitor concentrations in spite of the significant homology between these protein tyrosine kinases.These results demonstrate the ability to synthesize selective tyrosine kinase inhibitors.The most potent EGF receptor kinase inhibitors also inhibit the EGF-dependent proliferation of A431/clone 15 cells with little or no effect on EGF independent cell growth.These results demonstrate the potential use of protein tyrosine kinase inhibitors as selective antiproliferative agents for proliferative diseases caused by the hyperactivity of protein tyrosine kinases.We have suggested the name "tyrphostins" for this class of antiproliferative compounds which act as protein tyrosine kinase blockers.