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Rho Inhibitors (21)
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New Rho Products

Catalog No.	Product Name	Information	Product Use Citations
E2385^New	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.
E2400^New	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.
S0890	MLS000532223	MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM.
S1314	Zoledronic acid (ZOL 446)	Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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.	PLoS Pathog, 2022, 18(2):e1010299 J Bone Miner Res, 2022, 10.1002/jbmr.4507 Cancer Genomics Proteomics, 2022, 19(3):328-338
S1573	Fasudil (HA-1077) HCl	Fasudil (HA-1077, AT-877), 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.	Aging Cell, 2022, e13587 Cell Death Dis, 2022, 13(2):138 iScience, 2022, 25(6):104398
S1721	Azathioprine	Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.	Sci Rep, 2019, 9(1):4360 Blood, 2016, 1;128(9):1234-45
S3233	Emetine hydrochloride	Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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 Bone Miner Res, 2022, 10.1002/jbmr.4507 Oncol Lett, 2022, 23(2):51 Biomater Sci, 2021, 10.1039/d0bm02107e
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.
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.
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).
S6875^New	CASIN	CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
S7293	ZCL278	ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	J Clin Med, 2021, 10(13)2790 Front Oncol, 2021, 11:656608 EBioMedicine, 2019, 50:122-134
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.	Cancer Lett, 2022, 524:245-258 Cell Signal, 2022, S0898-6568(22)00031-6 PLoS Biol, 2021, 19(4):e3001134
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.	Small, 2021, 10.1002/smll.202104034 J Appl Toxicol, 2021, 10.1002/jat.4175 Cell, 2020, 182(3):685-712.e19
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.	Sci Adv, 2022, 8(15):eabm3471 Mol Ther Oncolytics, 2022, 24:873-886 Cell Transplant, 2022, 31:9636897221075749
S7719	CCG-1423	CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Adv Sci (Weinh), 2022, e2200053 Cell Transplant, 2022, 31:9636897221075749 Oncogene, 2021, 10.1038/s41388-021-02101-z
S8031	NSC 23766	NSC 23766 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.	Cell Death Discov, 2022, 8(1):26 Cell Transplant, 2022, 31:9636897221075749 Inflamm Res, 2022, 71(2):191-204
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.	J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
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.	Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8 Mol Cancer, 2021, 20(1):77 Cell, 2020, 182(3):685-712.e19
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.	Carcinogenesis, 2022, bgac014
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.
E0102^New	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.
E2385^New	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.
E2400^New	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.
S0890	MLS000532223	MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM.
S1314	Zoledronic acid (ZOL 446)	Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), 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.	PLoS Pathog, 2022, 18(2):e1010299 J Bone Miner Res, 2022, 10.1002/jbmr.4507 Cancer Genomics Proteomics, 2022, 19(3):328-338
S1573	Fasudil (HA-1077) HCl	Fasudil (HA-1077, AT-877), 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.	Aging Cell, 2022, e13587 Cell Death Dis, 2022, 13(2):138 iScience, 2022, 25(6):104398
S1721	Azathioprine	Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.	Sci Rep, 2019, 9(1):4360 Blood, 2016, 1;128(9):1234-45
S3233	Emetine hydrochloride	Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
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 Bone Miner Res, 2022, 10.1002/jbmr.4507 Oncol Lett, 2022, 23(2):51 Biomater Sci, 2021, 10.1039/d0bm02107e
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.
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.
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).
S6875^New	CASIN	CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
S7293	ZCL278	ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	J Clin Med, 2021, 10(13)2790 Front Oncol, 2021, 11:656608 EBioMedicine, 2019, 50:122-134
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.	Cancer Lett, 2022, 524:245-258 Cell Signal, 2022, S0898-6568(22)00031-6 PLoS Biol, 2021, 19(4):e3001134
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.	Small, 2021, 10.1002/smll.202104034 J Appl Toxicol, 2021, 10.1002/jat.4175 Cell, 2020, 182(3):685-712.e19
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.	Sci Adv, 2022, 8(15):eabm3471 Mol Ther Oncolytics, 2022, 24:873-886 Cell Transplant, 2022, 31:9636897221075749
S7719	CCG-1423	CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Adv Sci (Weinh), 2022, e2200053 Cell Transplant, 2022, 31:9636897221075749 Oncogene, 2021, 10.1038/s41388-021-02101-z
S8031	NSC 23766	NSC 23766 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.	Cell Death Discov, 2022, 8(1):26 Cell Transplant, 2022, 31:9636897221075749 Inflamm Res, 2022, 71(2):191-204
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.	J Cell Physiol, 2020, 235(5):4790-4803 Small GTPases, 2020, 10.1080/21541248
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.	Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8 Mol Cancer, 2021, 20(1):77 Cell, 2020, 182(3):685-712.e19
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.	Carcinogenesis, 2022, bgac014
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.
E0102^New	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.
E2385^New	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.
E2400^New	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.
S6875^New	CASIN	CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
E0102^New	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.