Rho

SKLB-163 acts by downregulating RhoGDI, activating JNK-1 signaling pathway and caspase-3, and reducing phosphorylated Akt and p44/42 MAPK.

Digeranyl bisphosphonate (DGBP) is a potent geranylgeranyl pyrophosphate (GGPP) synthase inhibitor that impedes the geranyl pyrophosphorylation of Rac1 and induces autophagy without causing apoptosis.

CCG-222740 is an inhibitor of Rho/MRTF pathway

Rhosin hydrochloride is a specific inhibitor of the RhoA subfamily Rho GTPases and inhibits the RhoA-GEF interaction. Rhosin hydrochloride can significantly induce cell apoptosis without affecting cell cycle progression. [1]

ITX3 is a specific, non-toxic, active and selective TrioN RhoGEF inhibitor with IC50 of 76 μM. ITX3 has anticancer effects, inhibits trion mediated GTP exchange on RhoG and Rac1, inhibits NGF-mediated neurite growth in PC12 cells and REF52 fibroblast structure formation induced by trion.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

GGTI 2147 decreased Rac1 activity, down-regulated p65 expression, and ameliorated OGD/R-induced neuronal apoptosis.

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.

Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.

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.

EHT 1864 (EHT 1864 2HCl) is a Rac family GTPase inhibitor that blocks activation by direct binding to Rac1, Rac1b, Rac2, and Rac3 (Kd=40/50/60/250 nM). EHT 1864 inhibits Rac, Ras, and Tiam-induced growth transformation of NIH-3T3 fibroblasts.

1A-116 is a specific inhibitor of Rac1 .

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

pan activator of Ras-related GTPases

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.

CCG-257081 (MRTF/SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF/SRF) that acts by inhibiting the Rho/MRTF/SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models. CCG-257081 can be used in cancer prevention and fibrosis research.

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.

MLS000532223 is a selectiveRho family GTPases inhibitor(EC50 : 16 μM to 120 μM).

ZINC69391 (CysHHC10 acetate(1408311-03-4 free base)) is a selective inhibitor of Rac1 with antiproliferative and antimetastatic effects. ZINC69391 interferes with the interaction of Rac1 with Dock180, reduces Rac1-GTP levels and induces apoptosis.

Z62954982 (ZINC08010136) is a selective inhibitor of Rac1, which stunts the growth and branching of neurons.Z62954982 inhibits Rac1 activation and reduces proliferation, p38 phosphorylation, and IL-6 levels in pulmonary arterioles.

Bicyclomycin benzoate, an antibiotic, exhibits activity against a broad spectrum of Gram-negative/Gram-positive bacteria.

CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM).

SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.

Y16 is a G protein-coupled Rho GEFs inhibitor that synergizes with Rhosin/G04 to inhibit LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling. Y16 is also a specific inhibitor of LARG with a Kd of 76 nM.