EHop-016

Catalog No.S7319

For research use only.

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

CAS No. 1380432-32-5

Selleck's EHop-016 has been cited by 29 publications

Purity & Quality Control

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 MoHRSpVv[3Srb36gZZN{[Xl? MlrHNlQhcA>? NHXUTGhKdmirYnn0bY9vKG:oIGLhZ|EhcW5iaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{Bi\nSncjCyOEBpenNiYomgS{1NUVODIHHzd4F6NCCLQ{WwQVEvOSEQvF2= MWiyOFUzODl7OB?=
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-JNK / JNK ; Rac1 25389450 31314174
In vivo

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

Protocol (from reference)

Kinase Assay:

[1]

  • 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:

[1]

  • 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.

Animal Research:

[2]

  • Animal Models: KITD814V-bearing mice.
  • Dosages: 2.5 μM
  • Administration: KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 430.55
Formula

C25H30N6O

CAS No. 1380432-32-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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