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EHop-016
🥰Excellent
Catalog No. T2427Cas No. 1380432-32-5
Alias EHop 016
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.
EHop-016
🥰Excellent
Purity: 100%
Catalog No. T2427Alias EHop 016Cas No. 1380432-32-5
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | 38 € | In Stock | |
| 10 mg | 63 € | In Stock | |
| 25 mg | 122 € | In Stock | |
| 50 mg | 213 € | In Stock | |
| 100 mg | 334 € | In Stock | |
| 200 mg | 492 € | In Stock | |
| 500 mg | 787 € | In Stock | |
| 1 mL x 10 mM (in DMSO) | 41 € | In Stock |
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Purity:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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. |
| Targets&IC50 | Rac1:1.1 μM |
| 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. |
| 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. |
| 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) |
| Alias | EHop 016 |
| Molecular Weight | 430.55 |
| Formula | C25H30N6O |
| Cas No. | 1380432-32-5 |
| Smiles | CCn1c2ccccc2c2cc(Nc3ccnc(NCCCN4CCOCC4)n3)ccc12 |
| Relative Density. | 1.27 g/cm3 |
Storage & Solubility Information
| 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.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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