Home Cell Cycle Rho

Rho Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E2400 1A-116 1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes.
Cancers (Basel), 2025, 17(3)461
Zool Res, 2024, 45(2):367-380
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.
J Biol Chem, 2023, 299(6):104749
Carcinogenesis, 2022, bgac014
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).
Theranostics, 2025, 15(16):8202-8221
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) signaling 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 tumor growth in xenograft models. It exhibits potent inhibition of phenotypic characteristics of Rac signaling 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 signaling 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 inhibiton 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.
Stem Cell Res Ther, 2025, 16(1):597
Transl Oncol, 2025, 51:102209
J Immunother Cancer, 2024, 12(11)e009805
Verified customer review of Fasudil (HA-1077) Hydrochloride
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.
Nat Med, 2025, 10.1038/s41591-025-04054-2
bioRxiv, 2025, 2025.09.09.675147
Cells, 2024, 13(10)862
Verified customer review of Zoledronic acid (Zoledronate)
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.
J Immunother Cancer, 2022, 10(12)e005660
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Oncol Lett, 2022, 23(2):51
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 tumor cell lines.
Sci Rep, 2025, 15(1):1283
E0102 I-191 I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling 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.
Front Immunol, 2024, 15:1477072