EHop-016

SKU: orb1305498

Description

EHop-016

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1380432-32-5
• MW: 430.55
• Purity: 98.99%
• Formula: C₂₅H₃₀N₆O
• SMILES: CCn1c2ccccc2c2cc(Nc3ccnc(NCCCN4CCOCC4)n3)ccc12
• Target: Ras,Rho
• Solubility: DMSO:50 mg/mL (116.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.65 mM)

Bioactivity

• Target IC50:
  Rac1:1.1 μM
• In Vivo:
  In MDA-MB-435 cells, EHop-016 (2-5 μM) inhibits the binding of active VAV2 to the Rac1 (G15A) mutant fusion protein, leading to a reduction in Rac-regulated cellular functions, including the formation of lamellipodia and cell migration. Due to compensatory mechanisms, the inhibition of Rac by EHop-016 results in increased activity of the closely related Rho GTPase RhoA. Additionally, EHop-016 suppresses the viability of MDA-MB-435 cells (IC50: 10 μM). EHop-016 also inhibits the growth induced by KITD814V in cells derived from SM and AML patients.
• In Vitro:
  EHop-016 significantly improves the survival rate of leukemia mice with KIT^D814V^ cells.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

angiogenesis, Cdc42, inhibit, PAK1, migration, Inhibitor, EHop 016, EHop016, EHop-016, Rac1, Rac3, Ras, Vav2

Compound Identifiers

PubChem CID

51031035