| Name | EHop-016 |
| Description | EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3. |
| Cell Research | MDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells (from ATCC) are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.(Only for Reference) |
| Kinase Assay | Rac Activity Assays: Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines (from ATCC). Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit. |
| In vitro | EHop-016 significantly improves the survival rate of leukemia mice with KIT^D814V^ cells. |
| In vivo | In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits the binding of active VAV2 to the Rac1 (G15A) mutant fusion protein, leading to a reduction in Rac-regulated cellular functions, including the formation of lamellipodia and cell migration. Due to compensatory mechanisms, the inhibition of Rac by EHop-016 results in increased activity of the closely related Rho GTPase RhoA. Additionally, EHop-016 suppresses the viability of MDA-MB-435 cells (IC50: 10 μM). EHop-016 also inhibits the growth induced by KITD814V in cells derived from SM and AML patients. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (116.13 mM), Sonication is recommended.
|
| Keywords | Ras | EHop016 | migration | Vav2 | Cdc42 | PAK1 | inhibit | EHop-016 | Rac3 | Rac1 | angiogenesis | Inhibitor |
| Inhibitors Related | Adagrasib | (S)-AMG-510 | BI-2493 | CCG-257081 | Ketoconazole | SKLB-163 | MRTX1133 | Salirasib | RMC-6236 | (S)-(-)-Perillyl alcohol | CASIN | Sotorasib |
| Related Compound Libraries | Ferroptosis Compound Library | Anti-Colorectal Cancer Compound Library | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
