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Rho Signaling Pathways

Rho Products

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  • New Rho Products
Catalog No. Product Name Information Product Use Citations Product Validations
E2385New 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.
E2400New 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 Cdc42WT and Cdc42Q61L 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).
S6875New 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 Kd 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 Kd 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.
E0102New 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.
E2385New 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.
E2400New 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 Cdc42WT and Cdc42Q61L 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).
S6875New 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 Kd 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 Kd 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.
E0102New 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.
E2385New 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.
E2400New 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.
S6875New CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
E0102New 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.
Tags: Rho inhibitor|Rho agonist|Rho activator|Rho inducer|Rho antagonist|Rho signaling pathway|Rho assay kit