Tyrphostin 8 

Tyrphostin 8 is a tyrosine kinase, with an IC₅₀ of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC₅₀=21 μM)^[1][2][3].

Tyrphostin 8 (10-100 μM; pretreated for 20 min) blocks the Carbachol-initiated PKCδ tyrosine phosphorylation and ERK1/2 activation in parotid acinar cells^[1].
Tyrphostin 8 (10-100 μM) produces a rapid and large increase in the basal O₂ consumption of parotid acinar^[1].
Tyrphostin 8 (10-100 μM) reduces the parotid ATP content by ∼90% at the concentration of 100 μM^[1].
Tyrphostin 8 increases apical-to-basolateral transport of insulin-transferrin conjugate by enhancing transferrin receptor-mediated transcytosis in filter-grown Caco-2 cell monolayer^[2].

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

Tyrphostin 8 improves the glucose-lowering effect of Insulin-transferrin in Streptozotocin-induced diabetic rats^[2].

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

170.17

C₁₀H₆N₂O

3785-90-8

Solid

Light yellow to yellow

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

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Soltoff SP. Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling. J Biol Chem. 2004 Mar 19;279(12):10910-8.  [Content Brief]

  [2]. Xia CQ, et, al. Tyrphostin-8 enhances transferrin receptor-mediated transcytosis in Caco-2- cells and inreases hypoglycemic effect of orally administered insulin-transferrin conjugate in diabetic rats. Pharm Res. 2001 Feb;18(2):191-5.  [Content Brief]

  [3]. Martin BL. Inhibition of calcineurin by the tyrphostin class of tyrosine kinase inhibitors. Biochem Pharmacol. 1998 Aug 15;56(4):483-8.  [Content Brief]