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EHT 1864

3872 19 Citations 1 Review Datasheet / COA / SDS
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EHT 1864 | CAS No. 754240-09-0 | Rho GTPase Inhibitors
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Description: Potent Rac family inhibitor

Chemical Name: 5-(5-(7-(Trifluoromethyl)quinolin-4-ylthio)pentyloxy)-2-(morpholinomethyl)-4H-pyran-4-one dihydrochloride

Purity: ≥98%

Product Details
Citations (19)
Reviews (1)
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

Inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo.

Technical Data

M.Wt:
581.47
Formula:
C25H27F3N2O4S.2HCl
Solubility:
Soluble to 100 mM in water and to 75 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
754240-09-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research use only under license from ExonHit Therapeutics S.A.

Product Datasheets

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Citations for EHT 1864

The citations listed below are publications that use Tocris products. Selected citations for EHT 1864 include:

19 Citations: Showing 1 - 10

  1. RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance.
    Authors: Lionarons Et al.
    Cancer Cell  2019;36:68
  2. Myosin VI-Dependent Actin Cages Encapsulate Parkin-Positive Damaged Mitochondria.
    Authors: Kruppa Et al.
    Dev Cell  2018;44:484
  3. Induction of non-apoptotic programmed cell death by oncogenic RAS in human epithelial cells and its suppression by MYC overexpression.
    Authors: Dendo Et al.
    Carcinogenesis  2018;39:202
  4. Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry.
    Authors: Ford Et al.
    PLoS Pathog  2018;14:e1007051
  5. Extracellular matrix promotes clathrin-dependent endocytosis of prolactin and STAT5 activation in differentiating mammary epithelial cells.
    Authors: Bridgewater Et al.
    Sci Rep  2017;7:4572
  6. Unravelling the Mechanism of TrkA-Induced Cell Death by Macropinocytosis in Medulloblastoma Daoy Cells.
    Authors: Li Et al.
    Mol.Cell Biol.  2016;36:2596
  7. Ras-related C3 botulinum. Substrate (Rac) and Src Family Kinases (SFK) Are Proximal and Essential for Phosphatidylinositol 3-Kinase (PI3K) Activation in Natural Killer (NK) Cell-mediated Direct Cytotoxicity against Cryptococcus neoformans.
    Authors: Xiang Et al.
    J Biol Chem  2016;291:6912
  8. Deletion of Rac1GTPase in the Myeloid Lineage Protects against Inflammation-Mediated Kidney Injury in Mice.
    Authors: Nagase Et al.
    PLoS One  2016;11:e0150886
  9. Loss of the E3 ubiquitin ligase HACE1 results in enhanced Rac1 signaling contributing to breast cancer progression.
    Authors: Goka and Lippman
    Am J Physiol Lung Cell Mol Physiol  2015;34:5395
  10. P-REX1 creates a positive feedback loop to activate growth factor receptor, PI3K/AKT and MEK/ERK signaling in breast cancer.
    Authors: Dillon Et al.
    Oncogene  2015;34:3968

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Rac inhibitor
By Anonymous on 01/31/2018
Application: Species: Mouse

Used to block Rac but no effect seen. Can't say if the compound actually works or not.

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