EHT 1864 2HCl

SKU: orb1300729

Description

EHT 1864

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 754240-09-0
• MW: 581.47
• Purity: 99.42%
• Formula: C₂₅H₂₉Cl₂F₃N₂O₄S
• SMILES: Cl.Cl.FC(F)(F)c1ccc2c(SCCCCCOc3coc(CN4CCOCC4)cc3=O)ccnc2c1
• Target: Ras,Rho

Bioactivity

• Target IC50:
  Rac2:60 nM(Kd)|Rac1b:50 nM(Kd)|Rac1:40 nM(Kd)|Rac3:250 nM(Kd)
• In Vivo:
  METHODS: To test the antitumor activity in vivo, EHT 1864 (100 mg/kg) was injected intraperitoneally twice daily for two weeks into NSG mice bearing BT-474 xenografts. RESULTS: EHT 1864 significantly slowed down tumor growth, with an average weekly growth rate of 50% vs. 27%. EHT 1864 greatly reduced the levels of P-ERK1/2, P-AKT, P-p70S6K, and P-Histone H3S10 (mitotic markers).
• In Vitro:
  METHODS: U87-MG cells were treated with EHT 1864 (10-25 µM) for 5 min and the levels of activated Rac1 or RhoA were measured by pull-down. RESULTS: EHT 1864 strongly inhibited the ability of Rac1 to interact with its effector Pak1 in a dose-dependent manner. In contrast, EHT 1864 did not affect the activation state of RhoA even at the highest dose tested (25 µM). METHODS: Mouse fibroblasts NIH 3T3 were treated with EHT 1864 (5 µM) for 4 h. Cultures were then stimulated with PDGF, LPA, or bradykinin for 15 min, fixed, and visualized for the actin filaments using Alexa phalloidin. RESULTS: PDGF, LPA and bradykinin were effective in inducing membrane wrinkling and lamellipodia formation, actin stress fibers and filamentous pseudopods, respectively. However, in the presence of EHT 1864, PDGF-induced lamellipodia formation was completely blocked, although LPA and bradykinin still induced their respective changes in actin cytoskeletal organization. EHT 1864-treated cells showed an approximately 80% reduction in lamellipodia stimulation by PDGF.
• Cell Research:
  NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ras, Rac1, Rac2, Rac3, Rac1b, precursor, transformation, EHT 1864, EHT1864, EHT-1864, amyloid, Alzheimer

Compound Identifiers

PubChem CID

9938202