Rho Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| E2400 | 1A-116 | 1A-116 is a Rac1 inhibitor, with antitumoural and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastatic processes. |
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| S8988 | Rhosin hydrochloride | Rhosin (G04) hydrochloride (HCl) is a potent, specific inhibitor of RhoA subfamily Rho GTPases with Kd of ~ 0.4 uM. Rhosin hydrochloride induces cell apoptosis. |
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| S6752 | Y16 | Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). |
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| S6875 | CASIN | CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. | ||
| E0345 | CCG-100602 | CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signalling that acts by blocking nuclear translocation of MRTF-A with an IC50 of 10 µM. | ||
| S6673 | CCG-222740 | CCG-222740 is a Rho/MRTF pathway inhibitor. This compound decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression. | ||
| E4622 | RP-102124 | RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. This compound is orally bioavailable and exhibits dose-dependent inhibition of tumour growth in xenograft models. It exhibits potent inhibition of phenotypic characteristics of Rac signalling such as cell migration and cytoskeletal rearrangements. | ||
| S5996 | MLS-573151 | MLS-573151 is a selective cell division cycle 42 (Cdc42) inhibitor with an EC50 of 2 μM, which acts by blocking the binding of GTP to Cdc42. | ||
| E2385 | SAR407899 hydrochloride | SAR407899 hydrochloride is a selective, potent and ATP-competitive Rho kinase (ROCK) inhibitor, with an IC50 of 135 nM for ROCK-2, and Ki values of 36 and 41 nM for human and rat ROCK-2, respectively. | ||
| S0890 | MLS000532223 | MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM. | ||
| E8045 | (R)-Ketorolac | (R)-Ketorolac ((+)-Ketorolac) is the R-enantiomer of ketorolac that functions as a selective allosteric inhibitor of the small GTPases Cdc42 and Rac1, blocking GTP binding and downstream signalling pathways like PAK activation. It exhibits the potential for repurposing as an anti-metastatic agent in ovarian cancer. | ||
| S1573 | Fasudil (HA-1077) Hydrochloride | Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibition over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
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| S1314 | Zoledronic acid (Zoledronate) | Zoledronic acid (Zoledronate), 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. Zoledronic acid (ZA) also induces autophagy. |
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| S5244 | Zoledronic acid monohydrate | Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which 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. |
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| S0765 | MAZ51 | MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumour cell lines. |
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| E0102 | I-191 | I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signalling pathways and functional responses. This compound also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88. |
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