2′-Thioadenosine (CAS 60239-18-1 (non-salt))

2'-Thioadenosine is a potent, selective, and irreversible inhibitor of the catalytic domain of the ErbB subfamily of protein tyrosine kinases. 2'-Thioadenosine inactivates epidermal growth factor receptor (ErbB1) via modification of a cysteine residue at the active site. This inactivation is reversed with the addition of 1mM dithiothreitol (DTT). 2'-Thioadenosine has also been shown to inhibit Neu/Her2 growth factor receptor (ErbB2, IC₅₀ = 45 µM).

References

1. Singh, J., et al., 1997. Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases. Journal of medicinal chemistry. 40(7): 1130-5. PMID: 9089334