DOCK is a family of related proteins involved in intracellular signalling networks. DOCK family members contain a RhoGEF domain to function as guanine nucleotide exchange factors to promote GDP release and GTP binding to specific Small GTPases of the Rho family (e.g., Rac and Cdc42), leading to their activation since Rho proteins are inactive when bound to GDP but active when bound to GTP.
|TBOPP is a selective DOCK1 inhibitor with IC50 value of 8.4μM. It dampened DOCK1-mediated invasion, macropinocytosis, and survival under the condition of glutamine deprivation. TBOPP treatment suppressed cancer metastasis and growth in vivo in mice.
|CPYPP is a DOCK2 inhibitor which bounds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. It also inhibits DOCK1 and DOCK5 and exhibits selectivity over DOCK9.