cdc42 gtpase

ZCL278 is a selective Cdc42 GTPase inhibitor.

ZCL279 is a small molecule modulator (SMM) that inhibits the interaction between CDC42 and intersectin (ITSN). At lower concentrations (<10 μM), ZCL279 activates Cdc42, a cytoplasmic small GTPase in the Ras superfamily, while at higher concentrations (<10 μM) it significantly inhibits it.

Rho GTPase inhibitor 1 (compound 7) is a potent inhibitor of Rho GTPase. It exhibits high affinity for Cdc42, Rac1, and RhoA, with dissociation constants (KDs) of 151 μM, 352 μM, and 232 μM, respectively. Additionally, Rho GTPase inhibitor 1 reduces cell migration in glioblastoma cell lines.

MLS-573151 is a selective inhibitor of GTPase Cdc42(EC50 of 2 μM). It is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42.

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

CASIN (Pirl1-related Compound 2) is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).

NSC 23766 is a Rac1 GTPase inhibitor that inhibits Rac1 activation by targeting guanine nucleotide exchange factors (GEFs), while it has no inhibitory effect on the closely related targets Cdc42 and RhoA, affecting the cell cycle and inhibiting cell proliferation in a dose-dependent manner. It also regulates endothelial NO synthase expression and endothelial function, and inhibits platelet aggregation and γ-secretase activity.NSC23766 competitively inhibits M2 muscarinic acetylcholine receptor (M2 mAChR)-induced Rac1 activation in neonatal rat cardiomyocytes.

NSC 23766 trihydrochloride (Rac1 Inhibitor) is an inhibitor of Rac GTPase targeting Rac activation by GEFs (IC50: ~50 μM); no inhibitory for the closely related targets, RhoA or Cdc42.

ARN22089 is an oral active CDC42 GTPase interaction inhibitor that blocks tumour growth in BRAF mutant mouse melanoma models and patient-derived xenografts (PDXs) in vivo.