EHT 1864, Rac family GTPase inhibitor (ab229172)

Overview

  • Product name

    EHT 1864, Rac family GTPase inhibitor
  • Description

    Potent Rac family GTPase inhibitor
  • Alternative names

    • EHT 1864 2HCl
  • Biological description

    EHT 1864 is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. In vitro it selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1. EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH/3T3 cells stably expressing H-Ras(61L) protein. EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down. It blocks breast cancer cell invasion in a collagen matrix assay and, at 10 µM, increases the size but decreases the density of dendritic spines of hippocampal neurons in culture. In vivo EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. Insoluble in ethanol.

  • Purity

    > 99%
  • CAS Number

    754240-09-0

Properties

  • Chemical name

    2-(4-Morpholinylmethyl)-5-[[5-[[7-(trifluoromethyl)-4-quinolinyl]thio]pentyl]oxy]-4H-pyran-4-one dihydrochloride
  • Molecular weight

    581.47
  • Molecular formula

    C25H27F3N2O4S.2HCl
  • PubChem identifier

    9938202
  • Storage instructions

    Shipped at 4°C. Store at -20°C long term. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 100 mM and in water to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C1COCCN1CC2=CC(=O)C(=CO2)OCCCCCSC3=C4C=CC(=CC4=NC=C3)C(F)(F)F.Cl.Cl
  • Source

    Synthetic

References

This product has been referenced in:

  • Kroon J  et al. Flow-induced endothelial cell alignment requires the RhoGEF Trio as a scaffold protein to polarize active Rac1 distribution. Mol Biol Cell 28:1745-1753 (2017). Read more (PubMed: 28515142) »
  • Raynaud F  et al. Rho-GTPase-activating protein interacting with Cdc-42-interacting protein 4 homolog 2 (Rich2): a new Ras-related C3 botulinum toxin substrate 1 (Rac1) GTPase-activating protein that controls dendritic spine morphogenesis. J Biol Chem 289:2600-9 (2014). Read more (PubMed: 24352656) »
  • Katz E  et al. Targeting of Rac GTPases blocks the spread of intact human breast cancer. Oncotarget 3:608-19 (2012). Read more (PubMed: 22689141) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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