An irreversible cysteine-targeting covalent inhibitor of Cdc42.
(A) Structure of DC-Rhoin04 bound to Cys107 (red) of RhoA (pink) (PDB 6KX3). Cdc42 (grey) displayed aligned to RhoA. (B) Crystal structure of K-RasG12C in complex with cysteine covalent inhibitor AMG 510 (PDB 6OIM), where AMG 510 binds to the switch II pocket of K-RasG12C in its inactive, GDP form exploiting a cryptic pocket formed by His95, Tyr96 and Gln99.