Rho
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1314 | Zoledronic Acid | <1 mg/mL | 0.004 mg/mL | <1 mg/mL |
| S8031 | NSC 23766 | 100 mg/mL | 100 mg/mL | <1 mg/mL |
| S7319 | EHop-016 | <1 mg/mL | 86 mg/mL | <1 mg/mL |
| S1721 | Azathioprine | <1 mg/mL | 54 mg/mL | <1 mg/mL |
| S7293 | ZCL278 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S8749 | MBQ-167 | <1 mg/mL | 68 mg/mL | 14 mg/mL |
| S5244 | Zoledronic acid monohydrate | <1 mg/mL | 0.01 mg/mL | <1 mg/mL |
| S7332 | K-Ras(G12C) inhibitor 9 | <1 mg/mL | 53 mg/mL | <1 mg/mL |
| S7719 | CCG-1423 | <1 mg/mL | 90 mg/mL | 4 mg/mL |
| S8469 | CCG-203971 | <1 mg/mL | 81 mg/mL | 4 mg/mL |
| S7330 | 6H05 | 100 mg/mL | 100 mg/mL | 100 mg/mL |
| S7331 | K-Ras(G12C) inhibitor 12 | <1 mg/mL | 27 mg/mL | <1 mg/mL |
| S8303 | Kobe0065 | <1 mg/mL | 89 mg/mL | 13 mg/mL |
| S7333 | K-Ras(G12C) inhibitor 6 | <1 mg/mL | 81 mg/mL | 30 mg/mL |
| S7607 | BQU57 | <1 mg/mL | 66 mg/mL | 20 mg/mL |
| S8499 | KRpep-2d | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S8156 | ARS-853 (ARS853) | <1 mg/mL | 86 mg/mL | 1 mg/mL |
| S7482 | EHT 1864 2HCl | 100 mg/mL | 100 mg/mL | <1 mg/mL |
| S7686 | ML141 | <1 mg/mL | 81 mg/mL | <1 mg/mL |
- Rho Inhibitors (20)
- New Rho Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1314 |
Zoledronic AcidZoledronic 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. |
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 meanSD from three experiments.*p<0.05, compared with no ZA.
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| S8031 |
NSC 23766NSC 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. |
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.
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| S7319 |
EHop-016EHop-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. |
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).
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| S1721 |
AzathioprineAzathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases. |
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| S7293 |
ZCL278ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM. |
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. |
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| S8749New |
MBQ-167MBQ-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. |
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| S5244New |
Zoledronic acid monohydrateZoledronic 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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| S7332 |
K-Ras(G12C) inhibitor 9K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
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| S7684 |
SalirasibSalirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2. |
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| S7719 |
CCG-1423CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription. |
Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
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| S8469 |
CCG-203971CCG-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. |
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| S7330 |
6H056H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C). |
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| S7331 |
K-Ras(G12C) inhibitor 12K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). |
-inhibitor-12-S733101W0420171213.gif)
-inhibitor-12-S733101W0420171213.gif)
(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.
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| S8303 |
Kobe0065Kobe0065 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. |
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| S7333 |
K-Ras(G12C) inhibitor 6K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
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| S7607 |
BQU57BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA. |
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| S8499 |
KRpep-2dKRpep-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. |
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| 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. |
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| S7482 |
EHT 1864 2HClEHT 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. |
Inhibition of Rac1 activity by EHT 1864 blocks alignment under flow, whereas solvent control-treated ECs aligned in the direction of flow. Note that the inhibitor was present throughout the experiment, due to the closed system that is used for long-term flow experiments. Bar graph on the right shows percentage of aligned cells in under static and flow conditions for both EHT 1864-treated and solvent-treated Ctrl ECs. ECs orientated between a 0-45° angle are quantified as being aligned. Data are mean of three independent experiments ± SEM. ***P<0.001. Bar, 25μm.
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| S7686 |
ML141ML141 (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.
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