| Bioactivity | 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]. |
| Invitro | 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]. Western Blot Analysis[1] Cell Line: |
| In Vivo | Tyrphostin 8 improves the glucose-lowering effect of Insulin-transferrin in Streptozotocin-induced diabetic rats[2]. |
| Name | Tyrphostin 8 |
| CAS | 3785-90-8 |
| Formula | C10H6N2O |
| Molar Mass | 170.17 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [3]. Martin BL. Inhibition of calcineurin by the tyrphostin class of tyrosine kinase inhibitors. Biochem Pharmacol. 1998 Aug 15;56(4):483-8. |