Tyrphostin A9  (Synonyms: Tyrphostin 9; Malonoben)

Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.

Tyrphostin A9 inhibited TNF-induced tyrosine phosphorylation of pyk2 without blocking the cells' bactericidal activity. Tyrphostin A9 is a PDGF receptor tyrosine kinase inhibitor (IC50 = 500 nM). Recent findings suggest that signaling via PDGF receptor tyrosine kinases is not necessary for the shift of the smooth muscle cells from a contractile to a synthetic phenotype. On the other hand these enzymes apparently carry out important functions in the control of intracellular membrane traffic and cell division.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

282.38

Solid

C₁₈H₂₂N₂O

10537-47-0

N#C/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1

Room temperature in continental US; may vary elsewhere.

• [1]. Park SJ, Park YJ, Shin JH, et al. A receptor tyrosine kinase inhibitor, Tyrphostin A9 induces cancer cell death through Drp1 dependent mitochondria fragmentation. Biochem Biophys Res Commun. 2011 May 13;408(3):465-70.  [Content Brief]

  [2]. Richard F. Loeser, Christopher B. Forsyth, Allen M. Samarel et al. Fibronectin Fragment Activation of Proline-rich Tyrosine Kinase PYK2 Mediates Integrin Signals Regulating Collagenase-3 Expression by Human Chondrocytes through a Protein Kinase C-dependen

  [3]. Michele Fuortes, Maxine Melchior, Hyunsil Han, et al. Role of the tyrosine kinase pyk2 in the integrin-dependent activation of human neutrophils by TNF. J Clin Invest. 1999;104(3):327-335.

  [4]. Johan Thyberg . Tyrphostin A9 and wortmannin perturb the Golgi complex and block proliferation of vascular smooth muscle cells. European Journal of Cell Biology.1998,76(1): 33-42

  [5]. R Marhaba, F Mary, C Pelassy, et al. Tyrphostin A9 inhibits calcium release-dependent phosphorylations and calcium entry via calcium release-activated channel in Jurkat T cells. The Journal of Immunology. 1996,157 (4): 1468-1473

  [6]. Kumar N, et al. Receptor tyrosine kinase inhibitors block multiple steps of influenza a virus replication. J Virol. 2011 Mar;85(6):2818-2  [Content Brief]