AG-537

AG-537 is a dimeric tyrphostin inhibitor of EGFR (IC₅₀ = 0.4 µM).¹ It is selective for EGFR over the Bcr-Abl fusion proteins p210 and p185 and wild-type c-Abl (IC₅₀s = 44, >100, and >100 µM, respectively, for the human proteins). AG-537 inhibits EGFR autophosphorylation (IC₅₀ = 3.3 µM) and EGF-dependent proliferation of HER14 fibroblasts (IC₅₀ = 3 µM).² It is also an inhibitor of T. brucei RNA-editing ligase 1 (REL1; IC₅₀ = 0.25 µM) and M. tuberculosis 4’-phosphopantetheinyl transferase (PptT; EC₅₀ = 5.9 µM in an apo-blue pigment synthetase A (BpsA) activation assay).^3,4

WARNING This product is not for human or veterinary use.

1. Anafi, M., Gazit, A., Gilon, C., et al. Selective interactions of transforming and normal abl proteins with ATP, tyrosine-copolymer substrates, and tyrphostins. The Journal of Biological Chemisty 267(8), 4518-4523 (1992).

2. Gazit, A., Osherov, N., Gilon, C., et al. Tyrphostins. 6. Dimeric benzylidenemalononitrile tyrphostins: Potent inhibitors of EGF receptor tyrosine kinase in vitro. J. Med. Chem. 39, 4905-4911 (1996).

3. Zimmermann, S., Hall, L., Riley, S., et al. A novel high-throughput activity assay for the Trypanosoma brucei editosome enzyme REL1 and other RNA ligases. Nucleic Acids Res. 44(3), e24 (2016).

4. Brown, A.S., Owen, J.G., Jung, J., et al. Inhibition of indigoidine synthesis as a high-throughput colourimetric screen for antibiotics targeting the essential Mycobacterium tuberculosis phosphopantetheinyl transferase PptT. Pharmaceuticals 13(7), 1066 (2021).