EHop-016

Catalog No.S7319

EHop-016  Chemical Structure

Molecular Weight(MW): 430.55

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.

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2 Customer Reviews

  • 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).

    Biochem Pharmacol, 2016, 105:42-54.. EHop-016 purchased from Selleck.

    (f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis.

    Cell Death Dis, 2015, 6:e1751.. EHop-016 purchased from Selleck.

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Choose Selective Rho Inhibitors

Biological Activity

Description 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.
Targets
Rac1 [1]
(MDA-MB-435, MDA-MB-231 cells)
1.1 μM
In vitro

Rac inhibition by EHop-016 increases the activity of the closely related Rho GTPase RhoA by a compensatory mechanism. In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits association of active Vav2 with Rac1(G15A) mutant fusion protein, and reduces Rac-regulated cell functions including lamellipodia formation and cell migration. In addition, EHop-016 inhibits cell viability of MDA-MB-435 cells with IC50 of 10 μM. [1] EHop-016 also inhibits KITD814V-induced growth in SM and AML patients-derived cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-435 cells M3\xZWZ2dmO2aX;uJIF{e2G7 MnO5NlQhcA>? M{mzNWlvcGmkaYTpc44hd2ZiUnHjNUBqdiCqdX3hckBOTEFvTVKtOFM2KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDHMWxKW0FiYYPzZZktKEmFNUC9NU4yKM7:TR?= Ml;FNlQ2OjB7OUi=

... Click to View More Cell Line Experimental Data

In vivo Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. [2]

Protocol

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • Cell lines: MDA-MB-231, MDA-MB-435, or MCF-10A cells
  • Concentrations: ~10 μM
  • Incubation Time: 24 hours
  • Method: 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)
Animal Research:[2]
+ Expand
  • Animal Models: KITD814V-bearing mice.
  • Formulation: DMSO
  • Dosages: 2.5 μM
  • Administration: KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 430.55
Formula

C25H30N6O

CAS No. 1380432-32-5
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID