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Rho

Isoform-selective Products

Cdc42-subclass Rac Rho-subclass

Signaling Pathway

Rho Products

All (25)
Rho Inhibitors (24)
Rho Activator (1)
New Rho Products

Catalog No.	Product Name	Information	Product Use Citations
S8031	NSC 23766 trihydrochloride	NSC 23766 trihydrochloride is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.	Nat Commun, 2024, 15(1):8159 Genes Dis, 2024, 11(3):101035 Neurobiol Stress, 2024, 32:100666
S1573	Fasudil HCl	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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
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.	Cells, 2024, 13(10)862 Cells, 2024, 13(10)862 Cancer Immunol Immunother, 2024, 73(4):62
S7319	EHop-016	EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3.	Microbiol Spectr, 2024, 12(1):e0239123 Theranostics, 2023, 13(2):543-559 JCI Insight, 2023, 8(9)e163864
S7719	CCG-1423	CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Cell Rep, 2024, 43(4):113989 Bioact Mater, 2023, 26:413-424 Genome Biol, 2023, 24(1):20
S7686	ML141	ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.	J Nanobiotechnology, 2024, 22(1):357 Genes Cancer, 2024, 15:15-27 Exp Mol Med, 2023, 55(4):779-793
S7482	EHT 1864 2HCl	EHT 1864 2HCl is a potent Rac family GTPase inhibitor with K_d of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.	Nat Commun, 2024, 15(1):2989 Dev Cell, 2024, S1534-5807(24)00175-8 Cell Rep, 2024, 43(8):114528
S7293	ZCL278	ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Cancer Commun (Lond), 2023, 43(8):909-937 J Exp Clin Cancer Res, 2022, 41(1):230 Front Oncol, 2021, 11:656608
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
S8749	MBQ-167	MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.	Nat Genet, 2022, 10.1038/s41588-022-01191-z Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8 Mol Cancer, 2021, 20(1):77
S8469	CCG-203971	CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.	Biomedicines, 2023, 11(9)2351 J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
S1721	Azathioprine	Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 Cell Rep, 2024, 43(8):114528
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 J Biol Chem, 2023, 299(6):104749 Carcinogenesis, 2022, bgac014
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 Cdc42^WT and Cdc42^Q61L mutant in GTP binding assay, respectively.	J Extracell Vesicles, 2024, 13(4):e12426 bioRxiv, 2023, 2023.07.23.550205
S6875	CASIN	CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
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.
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. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.
E4622^New	RP-102124	RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 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.
E0102	I-191	I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
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.
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.	Zool Res, 2024, 45(2):367-380
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.
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).
S8031	NSC 23766 trihydrochloride	NSC 23766 trihydrochloride is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.	Nat Commun, 2024, 15(1):8159 Genes Dis, 2024, 11(3):101035 Neurobiol Stress, 2024, 32:100666
S1573	Fasudil HCl	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.	Sci China Life Sci, 2024, 67(8):1549-1562 Ren Fail, 2024, 46(2):2396455 PeerJ, 2023, 11:e15494
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.	Cells, 2024, 13(10)862 Cells, 2024, 13(10)862 Cancer Immunol Immunother, 2024, 73(4):62
S7319	EHop-016	EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3.	Microbiol Spectr, 2024, 12(1):e0239123 Theranostics, 2023, 13(2):543-559 JCI Insight, 2023, 8(9)e163864
S7719	CCG-1423	CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Cell Rep, 2024, 43(4):113989 Bioact Mater, 2023, 26:413-424 Genome Biol, 2023, 24(1):20
S7686	ML141	ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.	J Nanobiotechnology, 2024, 22(1):357 Genes Cancer, 2024, 15:15-27 Exp Mol Med, 2023, 55(4):779-793
S7482	EHT 1864 2HCl	EHT 1864 2HCl is a potent Rac family GTPase inhibitor with K_d of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.	Nat Commun, 2024, 15(1):2989 Dev Cell, 2024, S1534-5807(24)00175-8 Cell Rep, 2024, 43(8):114528
S7293	ZCL278	ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Cancer Commun (Lond), 2023, 43(8):909-937 J Exp Clin Cancer Res, 2022, 41(1):230 Front Oncol, 2021, 11:656608
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
S8749	MBQ-167	MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.	Nat Genet, 2022, 10.1038/s41588-022-01191-z Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8 Mol Cancer, 2021, 20(1):77
S8469	CCG-203971	CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.	Biomedicines, 2023, 11(9)2351 J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
S1721	Azathioprine	Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 Cell Rep, 2024, 43(8):114528
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 J Biol Chem, 2023, 299(6):104749 Carcinogenesis, 2022, bgac014
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 Cdc42^WT and Cdc42^Q61L mutant in GTP binding assay, respectively.	J Extracell Vesicles, 2024, 13(4):e12426 bioRxiv, 2023, 2023.07.23.550205
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. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression.
E4622^New	RP-102124	RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 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.
E0102	I-191	I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
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.
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.	Zool Res, 2024, 45(2):367-380
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.
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).
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.
E4622^New	RP-102124	RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 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.

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