MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM. Small GTPases are key regulators of cellular activity .

BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA.

ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 μM and inhibits TrioN-stimulated RhoG exchange in vitro.

Rhosin HCl is a specific Rho inhibitor which binds to WT RhoA with an affinity ~0.4 μM Kd while does not interfere with the binding of Cdc42 or Rac1.

ML-098 is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM

CCG-1423 inhibits RhoA/C-mediated gene transcription and the invasion of rho-overexpressing cell lines.

Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.

Y16 is an inhibitor of G-protein–coupled Rho GEFs and works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras (G12C).

Rho-Kinase-IN-1 is a rho kinase inhibitor extracted from US 20090325960 A1, compound 1.008.

CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.

Zoledronic acid, a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.

CCG-222740 is a Rho/MRTF pathway inhibitor. It decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin (α-SMA) expression. It also modulates inflammatory components of the pancreas in KC mice (LSL-KrasG12D/+; Pdx-1-Cre) stimulated with caerulein.

Rhosin is a specific Rho inhibitor which binds to WT RhoA with an affinity ~0.4 μM Kd while does not interfere with the binding of Cdc42 or Rac1.