AG-556

AG-556 is a tyrphostin inhibitor of EGFR (IC50 = 5 µM). It is selective for EGFR over HER2 (IC50 = >500 µM). AG-556 inhibits EGF-induced growth of HER14 cells (IC50 = 3 µM). It inhibits hydrogen peroxide-induced increases in intracellular calcium in HEK293 cells expressing human transient receptor potential melastatin 2 (TRPM2, IC50 = 0.94 µM), as well as HEK293 cells expressing human TRP ankyrin 1 (TRPA1) when used at a concentration of 3 µM. AG-556 (200 µg/animal per day) reduces the incidence, severity, and duration of disease in a mouse model of experimental autoimmune encephalomyelitis (EAE). It reduces edema, demyelination, and myeloperoxidase (MPO) activity, a marker of neutrophil infiltration, in spinal cord tissue, as well as improves motor function in a mouse model of extradural compression-induced spinal cord injury when administered at a dose of 10 mg/kg.Formal Name: (2E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-(4-phenylbutyl)-2-propenamide. CAS Number: 133550-41-1. Synonyms: Tyrphostin 56, Tyrphostin AG-556. Molecular Formula: C20H20N2O3. Formula Weight: 336.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 256, 363 nm. SMILES: O=C(NCCCCC1=CC=CC=C1)/C(C#N)=C/C2=CC(O)=C(C=C2)O. InChi Code: InChI=1S/C20H20N2O3/c21-14-17(12-16-9-10-18(23)19(24)13-16)20(25)22-11-5-4-8-15-6-2-1-3-7-15/h1-3,6-7,9-10,12-13,23-24H,4-5,8,11H2,(H,22,25)/b17-12+. InChi Key: GWCNJMUSWLTSCW-SFQUDFHCSA-N.