(1) Cdc42–GEF small molecule inhibitors: ZCL278, ZCL367, CASIN, NSC23766, AZA1, AZA197, Ehop-016, MBQ-167 and DC-Rhoin04 (2) Cdc42 nucleotide binding inhibitors: ML141, R-Ketorolac (3) Membrane binding inhibitors: Secramine-A (4) Cdc42-effector complex inhibitor: P7 peptide (5) Effector inhibitors: ACK (AIM-100, NVP-TAE684), MRCK (BDP8900, BDP9066, BDP5290), LIMK1/2 (LX7101) and PAK4 (KPT-9274, PF-3758309). PDB structures shown: Cdc42·GDP (PDB:1DOA), Cdc42 in complex with GEF region of Intersectin (PDB: 1KI1), Cdc42·GTP with GMPPNP nucleotide shown in red (PDB:1NF3), ACK1 kinase domain (PDB: 4HZR), MRCKα (PDB: 4AW2), PAK4 kinase domain in complex with LIMK1 substrate peptide (PDB: 6WLY).