Home Cell Cycle Rho inhibitor EHop-016 For research use only.

EHop-016

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.

EHop-016 Chemical Structure

EHop-016 Chemical Structure

CAS No. 1380432-32-5

Purity & Quality Control

EHop-016 Related Products

Signaling Pathway

Rho Signaling Pathways

Rho Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-435 cells Function assay 24 h Inhibition of Rac1 in human MDA-MB-435 cells after 24 hrs by G-LISA assay, IC50=1.1 μM 24520998
Click to View More Cell Line Experimental Data

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
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]
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. 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 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-JNK / JNK Rac1 25389450
In Vivo
In vivo

Treatment of KITD814V-bearing cells with EHop-016 significantly enhances the survival of leukemic mice. [2]
Animal Research Animal Models KITD814V-bearing mice.
Dosages 2.5 μM
Administration KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.

Chemical Information & Solubility

Molecular Weight 430.55 Formula

C25H30N6O
CAS No. 1380432-32-5 SDF Download EHop-016 SDF
Smiles CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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