DOCK2-IN-1 (compound 3), a CPYPP ( HY-110100 ) analogue, is an inhibitor of DOCK2 as well ( IC 50 =19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation