EHop-016
Based on 8 publication(s) in Google Scholar
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
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- Pureté : 99.38%
- CAS No.: 1380432-32-5
- Formule: C25H30N6O
- Masse moléculaire:430.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
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Publications Citing Use of MedChemExpress (MCE) EHop-016
More- Pharmacol Res. 2026 Jan:223:108072. [Abstract]
- J Exp Med. 2023 Mar 6;220(3):e20221316. [Abstract]
- Biochem Pharmacol. 2021 Feb:184:114399. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2026 Apr 15;1872(6):168261. [Abstract]
- Cancers (Basel). 2025 Jan 23;17(3):361. [Abstract]
- Appl Microbiol Biotechnol. 2018 Jul;102(14):5965-5975. [Abstract]
- Mol Oncol. 2019 Sep;13(9):2010-2030. [Abstract]
- bioRxiv. 2025 January 15.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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RT-PCR
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ELISA
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MCF7 | GI50 |
14 μM
Compound: EHop-016
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Growth inhibition of human MCF7 cells after 24 hrs by SRB assay
Growth inhibition of human MCF7 cells after 24 hrs by SRB assay
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[PMID: 29358027] |
| MDA-MB-231 | GI50 |
15 μM
Compound: EHop-016
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Growth inhibition of human MDA-MB-231 cells after 24 hrs by SRB assay
Growth inhibition of human MDA-MB-231 cells after 24 hrs by SRB assay
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[PMID: 29358027] |
In Vitro
EHop-016 (1-10 μM; 24 hours; MDA-MB-435 cells) treatment inhibits Rac1 and Rac3 activity. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) [1].
EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells[1].
EHop-016 affectes cell viability by down-regulating Akt and Jun kinase activities and c-Myc and Cyclin D expression, as well as increasing caspase 3/7 activities in metastatic cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-435 cells
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Concentration:1 μM, 2 μM, 4 μM, 5 μM, 10 μM
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Incubation Time:24 hours
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Result:The activity Rac3 was inhibited by 58%.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nu/nu mice (4-5 weeks old) injected with GFP-MDA-MB-435 cells[2]
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Dosage:10 mg/kg, 25 mg/kg
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Administration:Intraperitoneal injection; 3 times a week; for 55 days
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Result:Significantly reduced mammary fat pad tumor growth, metastasis, and angiogenesis.
Chemical Information
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CAS No. 1380432-32-5
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Appearance Solid
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Masse moléculaire 430.55
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Formule C25H30N6O
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Color Light yellow to yellow
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SMILES
CCN1C2=C(C3=C1C=CC=C3)C=C(NC4=NC(NCCCN5CCOCC5)=NC=C4)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Functional, synaptoproteomic and structural adaptations underlying sex-dependent traumatic stress susceptibility/resilience in the hippocampus. [Abstract]2026 Jan:223:108072. PMID: 41453670 -
J Exp Med
Repurposing a tricyclic antidepressant in tumor and metabolism disease treatment through fatty acid uptake inhibition. [Abstract]2023 Mar 6;220(3):e20221316. PMID: 36520461
EHop-016 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Mar 6;220(3):e20221316. [Abstract]
EHop-016 (0, 1, 2, 3, μM; 4 days) did not affect cell proliferation in MDAMB-231 cells.
EHop-016 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Mar 6;220(3):e20221316. [Abstract]
EHop-016 (2 μM; 24 h and incubated with BODIPY-C16 (2 μM) for 2 h or TMR-Dextran (1 mg/ml) for 1 h) reduced the uptake of BODIPY-C16 and TMR-Dextran in MDAMB-231 cells.
EHop-016 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2023 Mar 6;220(3):e20221316. [Abstract]
EHop-016 (2 μM; 24 h and then incubated with BODIPY-C16 (5 μM) for 30 min prior to TMR-Dextran (1 mg/ml) treatment for another 30 min) reduced the uptake of BODIPY-C16 and TMR-Dextran in MDAMB-231 cells.
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Biochem Pharmacol
DOCK2 contributes to endotoxemia-induced acute lung injury in mice by activating proinflammatory macrophages. [Abstract]2021 Feb:184:114399. PMID: 33382969
EHop-016 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Feb:184:114399. [Abstract]
EHop-016 (1 μM; 24 h) costimulated with LPS exhibited remarkably suppressed LPS-induced IL-1β and TNF-α in RAW264.7 cells.
EHop-016 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Feb:184:114399. [Abstract]
EHop-016 (1 μM; 24 h) costimulated with LPS exhibited remarkably suppressed LPS-induced IL-1β and TNF-α, IL-6 in RAW264.7 cells.
EHop-016 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Feb:184:114399. [Abstract]
EHop-016 (1 μM; 15 min) costimulated with LPS exhibited remarkably inhibited LPS-induced IKK-β phosphorylation in RAW264.7 cells.
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Biochim Biophys Acta Mol Basis Dis
2026 Apr 15;1872(6):168261. PMID: 41990488 -
Cancers (Basel)
RAC1-Amplified and RAC1-A159V Hotspot-Mutated Head and Neck Cancer Sensitive to the Rac Inhibitor EHop-016 In Vivo: A Proof-of-Concept Study. [Abstract]2025 Jan 23;17(3):361. PMID: 39941730 -
Appl Microbiol Biotechnol
Deacetylmycoepoxydiene is an agonist of Rac1, and simultaneously induces autophagy and apoptosis. [Abstract]2018 Jul;102(14):5965-5975. PMID: 29740674 -
Mol Oncol
RAC1 inhibition reverses cisplatin resistance in esophageal squamous cell carcinoma and induces downregulation of glycolytic enzymes. [Abstract]2019 Sep;13(9):2010-2030. PMID: 31314174 -
Solvant et solubilité
In Vitro:
DMSO : ≥ 32 mg/mL (74.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (23.23 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Scratch/Wound-Healing Migration Assay
The scratch/wound-healing migration assay measures collective migration of adherent cells into an experimentally created cell-free gap in a confluent monolayer. The readout is generated by imaging the gap immediately after scratching and at later time points, then quantifying reduction in wound area, wound width, or percentage closure as cells move into the denuded region. Gap closure reflects cell migration but may also include cell proliferation, so interpretation should distinguish migration-focused conditions from proliferation-driven closure when possible, such as by using short assay windows, serum-controlled conditions, cell counting, or proliferation controls reported in published protocols.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Chemotaxis Gradient Chamber Assay 1
The chemotaxis gradient chamber assay is based on the principle of observing directional cell migration in response to a stable, linear or quasi-linear concentration gradient of a chemoattractant formed between two fluid reservoirs separated by a narrow observation chamber. Cells placed within the chamber respond to the gradient by polarized movement toward higher chemoattractant concentrations, allowing quantification of chemotactic behavior in real time under microscopy. The classic Zigmond chamber design enables simultaneous visualization of gradient formation and individual cell trajectories, making it suitable for studying leukocyte chemotaxis and other motile cell types in vitro.
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Under-Agarose Cell Migration Assay
The under-agarose cell migration assay is a classical in vitro chemotaxis method designed to evaluate directed cell movement through a semi-solid agarose matrix toward soluble chemoattractant gradients, enabling visualization and quantification of leukocyte or motile cell migration in a confined 2D-like environment. In this system, cells and chemoattractants are placed in separate wells cut into an agarose gel, allowing diffusion-driven gradient formation that guides directional migration, which is typically assessed by measuring migration distance, cell morphology changes, and accumulation toward the chemoattractant source. This assay has been widely used to study neutrophil and leukocyte chemotaxis as a simple alternative to filter-based migration systems and allows direct microscopic observation of migrating cells under near-physiological confinement conditions.
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Neural Crest/Neuronal Cell Migration Explant Assay
Neural crest (NC) and neuronal cell migration explant assays are in vitro systems in which neural tube-derived tissues are cultured to allow premigratory or newly emigrated neural crest cells to undergo epithelial-to-mesenchymal transition (EMT), migrate away from the explant, and form a measurable radial outgrowth that reflects migratory capacity and environmental responsiveness. These assays typically quantify migration by measuring the expansion of cell outgrowth from neural tube or neural plate border explants over time, often comparing early and later timepoints to derive a migration index such as a radius ratio, which reflects net cell dispersal from the explant core. Neural tube explant cultures preserve key aspects of neural crest behavior, including EMT, migration, and early differentiation, making them suitable for assessing intrinsic migratory ability and extrinsic cue dependence. However, studies emphasize that migratory outgrowth from neural tube explants may include non-n
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Transwell/Boyden Chamber Migration Assay
The Transwell/Boyden chamber migration assay measures cell movement through a porous membrane separating an upper and lower chamber, usually after a chemoattractant gradient is established by placing cells in the upper chamber and chemoattractant-containing medium in the lower chamber. The readout is generated by quantifying cells that traverse the membrane and appear on the lower membrane surface or in the lower chamber, depending on whether the cell type is adherent or non-adherent. This assay reflects chemotactic or haptotactic migration rather than matrix invasion unless an extracellular-matrix barrier is added to the membrane.
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3D Collagen/Hydrogel Matrix Migration Assay
The 3D collagen/hydrogel matrix migration assay is based on embedding cells within or on top of a fibrillar collagen type I-rich three-dimensional matrix to model in vivo-like extracellular matrix (ECM) architecture, enabling analysis of cell migration through a physically and biochemically relevant scaffold. In contrast to 2D migration systems, cells in 3D matrices interact with fibrillar collagen networks, requiring coordinated adhesion remodeling and proteolytic or non-proteolytic deformation mechanisms to move through confined spaces, thereby providing a more physiologically relevant readout of invasive and migratory behavior in tissue-like environments. Cell movement in 3D collagen matrices is typically quantified by tracking single-cell trajectories, invasion depth, or matrix penetration over time, reflecting combined effects of cytoskeletal dynamics, cell-ECM adhesion turnover, and ECM remodeling. These systems are widely used to study tumor cell invasion and stromal cell motili
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Cell-Exclusion Zone Migration Assay
The Cell-Exclusion Zone (CEZ) migration assay is an in vitro 2D cell migration method in which a defined cell-free area is created using removable physical barriers such as silicone stoppers, allowing cells to be seeded around the barrier and subsequently migrate into the cleared zone after barrier removal. This approach enables quantification of collective cell migration by monitoring repopulation of the initially cell-free region over time using microscopy-based imaging. Compared with scratch-based wound healing assays, barrier-based exclusion methods are designed to avoid mechanical damage to the extracellular matrix and reduce injury-induced effects on boundary cells, thereby improving interpretability of migration behavior in vitro. The assay readout is typically the progressive reduction in the cell-free area or the number of cells invading the exclusion zone, reflecting coordinated cell motility relevant to physiological processes such as wound healing, epithelial repair, and ca
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Chemotaxis Gradient Chamber Assay 2
Chemotaxis gradient chamber assays measure directional cell migration in response to a soluble chemical gradient by imaging cells as they move across a defined observation region; the readout is generated from time-lapse cell trajectories, displacement toward the gradient, forward migration index, trajectory plots, rose/polar plots, and statistical tests of non-random directionality. The Dunn chamber is a direct-viewing glass chamber in which cells migrate across a bridge between control and chemoattractant wells, allowing observation of cells in a linear concentration gradient; related direct-viewing formats include the Insall chamber, which supports defined unidirectional gradients and high numerical-aperture microscopy, and the μ-Slide Chemotaxis chamber, which supports long-term live-cell imaging and gradient characterization with fluorescent dye.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Montalvo-Ortiz BL, et al. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem. 2012 Apr 13;287(16):13228-38. [Content Brief]
[2]. Castillo-Pichardo L, et al. The Rac Inhibitor EHop-016 Inhibits Mammary Tumor Growth and Metastasis in a Nude Mouse Model. Transl Oncol. 2014 Oct 24;7(5):546-55. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3226 mL | 11.6131 mL | 23.2261 mL | 58.0653 mL |
| 5 mM | 0.4645 mL | 2.3226 mL | 4.6452 mL | 11.6131 mL | |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3226 mL | 5.8065 mL | |
| 15 mM | 0.1548 mL | 0.7742 mL | 1.5484 mL | 3.8710 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1613 mL | 2.9033 mL | |
| 25 mM | 0.0929 mL | 0.4645 mL | 0.9290 mL | 2.3226 mL | |
| 30 mM | 0.0774 mL | 0.3871 mL | 0.7742 mL | 1.9355 mL | |
| 40 mM | 0.0581 mL | 0.2903 mL | 0.5807 mL | 1.4516 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4645 mL | 1.1613 mL | |
| 60 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.9678 mL |
EHop-016 Related Classifications
HY-12810 Related Classifications
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