tyrphostin ag808

Tyrphostin AG-808 is a 15-human lipoxygenase inhibitor.

I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.

Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.

Tyrphostin AG 528 (Tyrphostin B66) is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM).

Tyrphostin AG 112 is an inhibitor of EGFR phosphorylation.

Tyrphostin AG 1112 is a Bcr-Abl kinase blocker. It can activate the terminal differentiation of K562 cells and the purging of Ph+ cells.

Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

Tyrphostin AG 1288 is an effective inhibitor of Tyrosine Kinase. It suppresses the expression of ICAM1 and TNFα-mediated cytotoxicity in vitro.

Tyrphostin AG 568 promotes Tyrphostin-induced inhibition of p210bcr-abl tyrosine kinase activity. It also induces K562 to differentiate.

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.