Rho

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

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]

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.

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.

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

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.

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

pan activator of Ras-related GTPases

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.

1A-116 is a specific inhibitor of Rac1 .

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

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.

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

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

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.

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.

CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50: 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. This compound also inhibits PC-3 cell migration (IC50: 4.2 μM), as determined by a scratch wound assay. CCG-203971(CCG203971) causes no cytotoxicity when evaluated by the WST-1 assay. It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.

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.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

(E Z)-ZINC09659342 is an inhibitor of Lbc-Rho A interaction.

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.

YH-306 (TRV055 acetate ) is a modulator of the FAK signaling pathway that acts by suppressing colorectal tumor growth and metastasis.

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.

Y16 acetate(429653-73-6 free base) is a G-protein–coupled Rho GEFs inhibitor; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.

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.

Rac1 Inhibitor F56, control peptide acetate is a control peptide version of Rac1 Inhibitor; comprises residues 45-60 of Rac1 with Trp56 replaced by Phe. Does not affect GEF-Rac1 interaction.