EHop-016

Catalog No.S7319 Batch:S731902

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Technical Data

Formula

C25H30N6O
Molecular Weight 430.55 CAS No. 1380432-32-5
Solubility (25°C)* In vitro DMSO 86 mg/mL (199.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.45mg/ml Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 Assay:

[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 Study:

[2]
  • Animal Models

    KITD814V-bearing mice.

  • Dosages

    2.5 μM

  • Administration

    KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection.

Customer Product Validation

, , Cell Death Dis, 2015, 6:e1751.

Data from [Data independently produced by , , Biochem Pharmacol, 2016, 105:42-54.]

Data from [Data independently produced by , , Exp Cell Res, 2017, 361(1):112-125]

Selleck's EHop-016 has been cited by 36 publications

Vav proteins do not influence dengue virus replication but are associated with induction of phospho-ERK, IL-6, and viperin mRNA following DENV infection in vitro [ Microbiol Spectr, 2024, 12(1):e0239123] PubMed: 38054722
Sigma-1 receptor-regulated efferocytosis by infiltrating circulating macrophages/microglial cells protects against neuronal impairments and promotes functional recovery in cerebral ischemic stroke [ Theranostics, 2023, 13(2):543-559] PubMed: 36632219
Loss of Dnmt3a impairs hematopoietic homeostasis and myeloid cell skewing via the PI3Kinase pathway [ JCI Insight, 2023, 8(9)e163864] PubMed: 36976647
Loss of Dnmt3a impairs hematopoietic homeostasis and myeloid cell skewing via the PI3Kinase pathway [ JCI Insight, 2023, 8(9)e163864] PubMed: 36976647
ATM inhibition drives metabolic adaptation via induction of macropinocytosis [ J Cell Biol, 2023, 222(1)e202007026] PubMed: 36399181
Activation of the mevalonate pathway in response to anti-cancer treatments drives glioblastoma recurrences through activation of Rac-1 [ bioRxiv, 2023, 2023.07.23.550205] PubMed: 37546917
Non-muscle myosin II isoforms orchestrate substrate stiffness sensing to promote cancer cell contractility and migration [ Cancer Lett, 2022, 524:245-258] PubMed: 34715250
Gas6 Promotes Microglia Efferocytosis and Suppresses Inflammation Through Activating Axl/Rac1 Signaling in Subarachnoid Hemorrhage Mice [ Transl Stroke Res, 2022, 10.1007/s12975-022-01099-0] PubMed: 36324028
LncRNA RP11-214F16.8 drives breast cancer tumorigenesis via a post-translational repression on NISCH expression [ Cell Signal, 2022, S0898-6568(22)00031-6] PubMed: 35108640
Farnesyl pyrophosphate is a new danger signal inducing acute cell death [ PLoS Biol, 2021, 19(4):e3001134] PubMed: 33901180

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.