EHT 1864
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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%
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.
Background References
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RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo.
Desire et al.
J.Biol.Chem., 2005;280:37516 -
Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases.
Shutes et al.
J.Biol.Chem., 2007;282:35666 -
Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases.
Onesto et al.
Methods Enzymol., 2008;439:111
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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
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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
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Myosin VI-Dependent Actin Cages Encapsulate Parkin-Positive Damaged Mitochondria.
Authors: Kruppa Et al.
Dev Cell 2018;44:484
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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
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Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry.
Authors: Ford Et al.
PLoS Pathog 2018;14:e1007051
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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
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Unravelling the Mechanism of TrkA-Induced Cell Death by Macropinocytosis in Medulloblastoma Daoy Cells.
Authors: Li Et al.
Mol.Cell Biol. 2016;36:2596
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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
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Deletion of Rac1GTPase in the Myeloid Lineage Protects against Inflammation-Mediated Kidney Injury in Mice.
Authors: Nagase Et al.
PLoS One 2016;11:e0150886
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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
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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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Inhibition of prostate smooth muscle contraction and prostate stromal cell growth by the inhibitors of Rac, NSC23766 and EHT1864.
Authors: Wang Et al.
Br J Pharmacol 2015;172:2905
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Albumin-associated free fatty acids induce macropinocytosis in podocytes.
Authors: Chung Et al.
J Clin Invest 2015;125:2307
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Rac1 is required for matrix metalloproteinase 13 production by chondrocytes in response to fibronectin fragments.
Authors: Long Et al.
Cell Cycle 2013;65:1561
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The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval.
Authors: Zhang Et al.
J Neurosci 2013;33:5006
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Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells.
Authors: Dipaolo Et al.
Microbiology 2013;305:L141
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Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration.
Authors: Gadepalli Et al.
Oncogene 2013;288:30815
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Inhibition of hepcidin transcription by growth factors.
Authors: Goodnough Et al.
Hepatology 2012;56:291
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Targeting of Rac GTPases blocks the spread of intact human breast cancer.
Authors: Katz Et al.
Oncotarget 2012;3:608
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Tannerella forsythia invasion in oral epithelial cells requires phosphoinositide 3-kinase activation and clathrin-mediated endocytosis.
Authors: Mishima and Sharma
Arthritis Rheum 2011;157:2382
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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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