EHT 1864

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    EHT 1864 is a small-molecule inhibitor of Rac family small GTPases with Kd value of 40nM for Rac1 [1].In NIH 3T3 mouse fibroblasts, EHT 1864 treatment shows an 80% reduction in PDGF-induced lamellipodia formation. EHT 1864 at concentration of 50μM can completely inhibit the complex formation between Rac1 and PAK-RBD and cause the release of nucleotide from Rac1. The reassociation of nucleotide with Rac1 induced by EDTA or the Tiam1 can also be blocked by EHT 1864. EHT 1864 is most potent to Rac1, both in the binding affinity and stimulation of nucleotide release. It binds to Rac1b, Rac2 and Rac3 with Kd values of 50nM, 60nM and 250nM, respectively. Moreover, EHT 1864 can suppress cellular transformation induced by Rac1 with an 80% inhibition of focus-forming activity [1].
    
    [1] Shutes A, Onesto C, Picard V, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Journal of Biological Chemistry, 2007, 282(49): 35666-35678.
- Properties
  - CAS Number
    
    754240-09-0
    
    Molecular Formula
    
    C25H29Cl2F3N2O4S
    
    Molecular Weight
    
    581.48
    
    Appearance
    
    A solid
    
    Purity
    
    99.68%
    
    Solubility
    
    ≥29.05 mg/mL in DMSO with gentle warming; ≥16.53 mg/mL in H2O; ≥2.1 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Jun Sun, Gabriel Gaidosh, et al. "RAC1 plays an essential role in estrogen receptor alpha function in breast cancer cells." Oncogene. 2021 Oct;40(40):5950-5962. PMID:34373577

EHT 1864

Background

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