Cdc42

AZA197 (AZA-197) is a selective Cdc42 inhibitor. It acts by inhibiting primary colon cancer growth and prolonging survival in a preclinical mouse xenograft model by downregulation of PAK1 activity.

AZA1 (Rac1 Cdc42-IN-1) is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induced apoptosis of prostate cancer cells and inhibited cell proliferation, migration and invasion.

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.

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

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.

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.

CID44216842 (KUC103479N-02) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

MBQ-167 is a dual inhibitor of Rac Cdc42 (IC50s: 103 nM for Rac 1 2 3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively).

Rhosin is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin causes cell apoptosis.

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.

2-Mc-1,4-NHQ, an inhibitor of the Cdc42-PBD interaction, blocks the association of Cdc42 with the PBD.

KRCA-0008 is an effective and specific ALK Ack1 inhibitor (IC50: 12 4 nM); displays drug-like properties without hERG liability.

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

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.

AIM-100 is a Ack1 inhibitor (IC50: 24 nM).

1. alpha-Cyperone (α-Cyperone) is a promising inhibitor of Hla production by S. aureus and protects lung cells from this bacterium. 2. alpha-Cyperone significantly inhibited PGE2 production by suppressing the LPS-induced expression of inducible COX-2 at both the mRNA and the protein levels , downregulated the production and mRNA expression of the inflammatory cytokine IL-6. 3. alpha-Cyperone inhibited actin cytoskeleton polymerization induced by APEC-O78 through down regulating the expression of Nck-2, Cdc42 and Rac1.

(R)-BDP9066 is a highly effective inhibitor of myotonic dystrophy kinase-related Cdc42-binding kinase (MRCK), effectively impeding cancer cell invasion, making it an invaluable resource for studying and researching proliferative diseases, particularly cancer.

NVP-TAC544 is a novel focal adhesion kinase (FAK) inhibitor, potently blocking kinase activity of FAK along with Aurora A, activated Cdc42-associated kinase 1 (ACK1), Met, insulin receptor (IR), TrkA, and IGF-1R.

Antiangiogenic agent 3 is a potent inhibitor of human umbilical vein endothelial cells (HUVEC), effectively blocking HUVEC migration and chemotactic motilities. Additionally, it suppresses the gene expression of Src, cdc42, and MAPK, manifesting its strong antiangiogenic properties.

ARN22089, an orally active novel class of trisubstituted pyrimidine, inhibits the interaction of CDC42 GTPases with specific downstream effectors and blocks tumor growth in a BRAF mutant mouse melanoma model [1].

ARN25062 is an inhibitor of the protein-protein interaction between Cdc42 and p21-activated kinase (PAK). It inhibits the proliferation of SKM28, SK-MEL-3, WM3248, and A375 melanoma cells (IC50s = 6.1, 4.6, 9.3, and 5.1 µM, respectively) and SW480 colon cancer cells (IC50 = 5.9 µM).