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Rho Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S6000 CID44216842 CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor with EC50s of 1.0 μM and 1.2 μM for Cdc42WT and Cdc42Q61L mutant in GTP binding assay, respectively.
Cancer Research Communications, June 25, 2024, 1566-1580
J Extracell Vesicles, 2024, 13(4):e12426
bioRxiv, 2023, 2023.07.23.550205
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
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
Theranostics, 2025, 8202-8221
The EMBO Journal, 2025, 1-20
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.
bioRxiv, March 20 2024, nan
Translational Vision Science & Technology, June 20 2017, 22
PeerJ, June 06 2023, e15494
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.
Cells, 2024, 862
J Immunother Cancer, 2022, 10(12)e005660
J Bone Miner Res, 2022, 10.1002/jbmr.4507
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
International Immunopharmacology, 2025, 114443
Human Molecular Genetics, 2014, 6553-6566
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