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Chemical Structure| 1380432-32-5 Chemical Structure| 1380432-32-5

Structure of EHop-016
CAS No.: 1380432-32-5

Chemical Structure| 1380432-32-5

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EHop-016 is an effective selective inhibitor of Rac GTPase Rac1 and Rac3. It inhibits Rac1 activity in MDA-MB-435 cells with an IC50 of 1.1 μM. EHop-016 inhibits the interaction of Vav2 with Rac, Rac-mediated PAK1 activation, lamellipodia formation, and cell migration.

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Product Details of EHop-016

CAS No. :1380432-32-5
Formula : C25H30N6O
M.W : 430.55
SMILES Code : CCN1C2=C(C3=C1C=CC=C3)C=C(NC4=NC(NCCCN5CCOCC5)=NC=C4)C=C2
MDL No. :MFCD23143628
InChI Key :AFTZZRFCMOAFCR-UHFFFAOYSA-N
Pubchem ID :51031035

Safety of EHop-016

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of EHop-016

GPCR

Isoform Comparison

Biological Activity

Target
  • Rac

    Rac1, IC50:1.1 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-435 cells 5, 10, 25 μM 24 hours EHop-016 significantly increases caspase 3/7 activity at concentrations ≥10μM, indicating it may induce apoptosis. PMC4225654
PC3 cells 8 μM 24 hours EHop-016 inhibits Rac activity in PC3 cells by 50%. PMC4225654
HUVEC cells 4, 8 μM 24 hours EHop-016 reduces tube formation in HUVEC cells at 4 μM, and significantly inhibits tube formation at 8 μM. PMC4225654

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice myxofibrosarcoma xenograft Oral gavage 15 mg/kg or 20 mg/kg twice daily 5 days per week until significant tumor inhibition Significant inhibition of tumor growth and lung metastasis PMC5050162
Nude mice Breast cancer model Intraperitoneal injection 10, 25 mg/kg 3 times a week for 8 weeks EHop-016 significantly reduces mammary fat pad tumor growth and metastasis, and inhibits angiogenesis. PMC4225654

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.61mL

2.32mL

1.16mL

23.23mL

4.65mL

2.32mL

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