Rho

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Inhibitory Selectivity

Rho Products

All (21) Rho Inhibitors (21) New Rho Products

Catalog No.	Information	Product Use Citations	Product Validations
S1314	Zoledronic Acid Zoledronic acid (ZA), 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.	Int J Cancer, 2016, 138(5):1281-9 Mol Cancer Ther, 2016, 15(5):854-65 J Mol Cell Cardiol, 2016, 99:76-86	Quantification (C) of SA-β-gal+ SMCs after sustained 100nM ADP treatment for 48hr with or without Ras inhibitor zoledronic acid (ZA) (n=4 in each group). #p<0.05, ##p<0.01 compared with control, p<0.05 compared with P2ry12+/+ADP. (D) Incidence of TAAD formation and rupture after BAPN administration with or without ZA. (E) Elastin degradation grades of mice aortas after BAPN administration with or without ZA. (F) Representative H&E staining of thoracic aorta and progression of thoracic aorta diameter of mice aortas after BAPN administration with or without ZA (n=8 in both group). (G) Representative images and quantification of SA-β-gal (blue) staining in mouse aorta after BAPN administration with or without ZA (n=4 in both group); arrow, location of SA-β-gal+ area. (H) Immunostaining and quantification of p-ERK and p-p38 in mouse aorta with or without ZA (n=4 in both group). Data are meanSD from three experiments.p<0.05, compared with no ZA.
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.	Cancer Lett, 2016, 10.1016/j.canlet.2016.02.049 Sci Signal, 2018, 11(528) Cell Death Dis, 2015, 6:e1751	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.	Cell Death Dis, 2015, 6:e1751 Biochem Pharmacol, 2016, 105:42-54 Exp Cell Res, 2017, 361(1):112-125	Human HCT116 cells were treated with conditioned media of (LPS + Chol)-treated THP-Ms or IL-1b (10 ng/ml) in the absence or presence of Ehop-016 (10 μM), and effects of the indicated factors on b-catenin transcriptional activity of HCT116 cells were determined by the TOP and FOP flash reporter assay, and the protein levels of GTP-Rac1, total Rac1, p-GSK3b (S9), total GSK3b, PCNA and Cyclin D1 were analyzed by western blot (H).
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.
S7293	ZCL278 ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Cell Physiol Biochem, 2015, 36(4):1613-1627 Biol Trace Elem Res, 2016, 170(1):173-82 J Cell Physiol, 2018, 10.1002/jcp.27510	Effect OF ZCL278 on activation of Jak1/2 and Stat3 by IL-1β. PACs were treated with IL-1β at 10 ng/ml for the indicated times or 1 h。
S8749^New	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.
S8707^New	ARS-1620 ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRAS^G12C and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
S7684	Salirasib Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with K_i of 2.6 μM, which inhibits _Ras methylation. Phase 2.
S7719	CCG-1423 CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Cell Signal, 2017, 31:87-95 Oncol Rep, 2018, 39(2):465-472 Biomed Pharmacother, 2018, 104:718-728	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.
S7330	6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).	Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
S7607	BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
S8499	KRpep-2d KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
S8156	ARS-853 (ARS853) ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
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.	Mol Biol Cell, 2017, 28(13):1745-1753 Int J Clin Exp Pathol, 2016, 9(6):5902-5911 Am J Cancer Res, 2018, 8(1):70-80	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).		(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.
S5244	Zoledronic acid monohydrate Zoledronic acid, 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.

Catalog No.	Information	Product Use Citations	Product Validations
S1314	Zoledronic Acid Zoledronic acid (ZA), 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.	Int J Cancer, 2016, 138(5):1281-9 Mol Cancer Ther, 2016, 15(5):854-65 J Mol Cell Cardiol, 2016, 99:76-86	Quantification (C) of SA-β-gal+ SMCs after sustained 100nM ADP treatment for 48hr with or without Ras inhibitor zoledronic acid (ZA) (n=4 in each group). #p<0.05, ##p<0.01 compared with control, p<0.05 compared with P2ry12+/+ADP. (D) Incidence of TAAD formation and rupture after BAPN administration with or without ZA. (E) Elastin degradation grades of mice aortas after BAPN administration with or without ZA. (F) Representative H&E staining of thoracic aorta and progression of thoracic aorta diameter of mice aortas after BAPN administration with or without ZA (n=8 in both group). (G) Representative images and quantification of SA-β-gal (blue) staining in mouse aorta after BAPN administration with or without ZA (n=4 in both group); arrow, location of SA-β-gal+ area. (H) Immunostaining and quantification of p-ERK and p-p38 in mouse aorta with or without ZA (n=4 in both group). Data are meanSD from three experiments.p<0.05, compared with no ZA.
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.	Cancer Lett, 2016, 10.1016/j.canlet.2016.02.049 Sci Signal, 2018, 11(528) Cell Death Dis, 2015, 6:e1751	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.	Cell Death Dis, 2015, 6:e1751 Biochem Pharmacol, 2016, 105:42-54 Exp Cell Res, 2017, 361(1):112-125	Human HCT116 cells were treated with conditioned media of (LPS + Chol)-treated THP-Ms or IL-1b (10 ng/ml) in the absence or presence of Ehop-016 (10 μM), and effects of the indicated factors on b-catenin transcriptional activity of HCT116 cells were determined by the TOP and FOP flash reporter assay, and the protein levels of GTP-Rac1, total Rac1, p-GSK3b (S9), total GSK3b, PCNA and Cyclin D1 were analyzed by western blot (H).
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.
S7293	ZCL278 ZCL278 is a selective Cdc42 GTPase inhibitor with K_d of 11.4 μM.	Cell Physiol Biochem, 2015, 36(4):1613-1627 Biol Trace Elem Res, 2016, 170(1):173-82 J Cell Physiol, 2018, 10.1002/jcp.27510	Effect OF ZCL278 on activation of Jak1/2 and Stat3 by IL-1β. PACs were treated with IL-1β at 10 ng/ml for the indicated times or 1 h。
S8749^New	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.
S8707^New	ARS-1620 ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRAS^G12C and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
S7684	Salirasib Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with K_i of 2.6 μM, which inhibits _Ras methylation. Phase 2.
S7719	CCG-1423 CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.	Cell Signal, 2017, 31:87-95 Oncol Rep, 2018, 39(2):465-472 Biomed Pharmacother, 2018, 104:718-728	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.
S7330	6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7331	K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).	Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
S8303	Kobe0065 Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
S7333	K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
S7607	BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
S8499	KRpep-2d KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
S8156	ARS-853 (ARS853) ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
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.	Mol Biol Cell, 2017, 28(13):1745-1753 Int J Clin Exp Pathol, 2016, 9(6):5902-5911 Am J Cancer Res, 2018, 8(1):70-80	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).		(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.
S5244	Zoledronic acid monohydrate Zoledronic acid, 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.

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Rho

Signaling Pathway Map

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Inhibitory Selectivity

Rho Products