Rho

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Rho Products

All (21) Rho Inhibitors (19) Rho Activators (1) Rho Antagonists (1)

Catalog No.	Information	Product Use Citations	Product Validations
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.	Proc Natl Acad Sci U S A, 2021, 118(2)e2016034118 J Neurochem, 2021, 10.1111/jnc.15436 Cell Regen, 2021, 10(1):8	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
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.	Biomater Sci, 2021, 10.1039/d0bm02107e Hum Cell, 2021, 10.1007/s13577-021-00579-z Aging Cell, 2020, 29	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
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.	Theranostics, 2021, 11(9):4316-4334 Elife, 2021, 10e65962 BMC Biol, 2021, 19(1):140	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
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.	PLoS Biol, 2021, 19(4):e3001134 PLoS Genet, 2020, 16(3):e1008694 Stem Cell Res Ther, 2020, 11(1):525	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
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
S6875^New	CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
S6000^New	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.
S7293	ZCL278 ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Front Oncol, 2021, 11:656608 EBioMedicine, 2019, 50:122-134 J Bone Miner Res, 2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
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.	Mol Cancer, 2021, 20(1):77 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
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.
S7719	CCG-1423 CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Front Cell Dev Biol, 2021, 9:664375 Front Cell Dev Biol, 2021, 9:583492 Microb Pathog, 2021, 158:105054	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
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
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.
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.
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.	J Appl Toxicol, 2021, 10.1002/jat.4175 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
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.	Cell Rep, 2021, 36(1):109254 FASEB J, 2021, 35(5):e21598 Sci Rep, 2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S0890	MLS000532223 MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM.
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.	Biomater Sci, 2021, 10.1039/d0bm02107e Cancers (Basel), 2020, 31;12(1) pii: E104 J Cell Mol Med, 2020, 25
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.
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.

Catalog No.	Information	Product Use Citations	Product Validations
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.	Proc Natl Acad Sci U S A, 2021, 118(2)e2016034118 J Neurochem, 2021, 10.1111/jnc.15436 Cell Regen, 2021, 10(1):8	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
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.	Biomater Sci, 2021, 10.1039/d0bm02107e Hum Cell, 2021, 10.1007/s13577-021-00579-z Aging Cell, 2020, 29	Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
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.	Theranostics, 2021, 11(9):4316-4334 Elife, 2021, 10e65962 BMC Biol, 2021, 19(1):140	MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
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.	PLoS Biol, 2021, 19(4):e3001134 PLoS Genet, 2020, 16(3):e1008694 Stem Cell Res Ther, 2020, 11(1):525	(f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.
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
S6875^New	CASIN CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM.
S6000^New	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.
S7293	ZCL278 ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Front Oncol, 2021, 11:656608 EBioMedicine, 2019, 50:122-134 J Bone Miner Res, 2018, 33(5):945-958	Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group.
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.	Mol Cancer, 2021, 20(1):77 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
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.
S7719	CCG-1423 CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Front Cell Dev Biol, 2021, 9:664375 Front Cell Dev Biol, 2021, 9:583492 Microb Pathog, 2021, 158:105054	Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
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
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.
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.
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.	J Appl Toxicol, 2021, 10.1002/jat.4175 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
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.	Cell Rep, 2021, 36(1):109254 FASEB J, 2021, 35(5):e21598 Sci Rep, 2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S0890	MLS000532223 MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM.
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.	Biomater Sci, 2021, 10.1039/d0bm02107e Cancers (Basel), 2020, 31;12(1) pii: E104 J Cell Mol Med, 2020, 25
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).

Catalog No.	Information	Product Use Citations	Product Validations
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.

Catalog No.

Information

Product Use Citations

Product Validations

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.

Catalog No.	Information	Product Use Citations	Product Validations
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.

Catalog No.

Information

Product Use Citations

Product Validations

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.

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