Fumosorinone is a novel potent, selective protein tyrosine phosphatase SHP2 inhibitor with IC50 of 6.31 uM.
Fumosorinone shows little to no inhibition toward other human PTPs (2-7 fold over PTP1B, TCPTP and SHP1).
Fumosorinone inhibits Shp2-dependent activation of the Ras/ERK signal pathway downstream of EGFR, and interrupts EGF-induced Gab1-Shp2 association.
Fumosorinone shows little effects on the Shp2-independent ERK1/2 activation induced by PMA or oncogenic Ras.
Fumosorinone down-regulates Src activation, inhibits phosphorylation of Paxillin and prevents tumor cell invasion.
Fumosorinone shows anti-diabetic effect in diabetic KKAy mice.
