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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.
Sold for research use only under license from ExonHit Therapeutics S.A.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 581.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.72 mL||8.6 mL||17.2 mL|
|5 mM||0.34 mL||1.72 mL||3.44 mL|
|10 mM||0.17 mL||0.86 mL||1.72 mL|
|50 mM||0.03 mL||0.17 mL||0.34 mL|
References are publications that support the biological activity of the product.
Desire et al (2005) RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo. J.Biol.Chem. 280 37516 PMID: 16150730
Shutes et al (2007) Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases. J.Biol.Chem. 282 35666 PMID: 17932039
Onesto et al (2008) Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 439 111 PMID: 18374160
If you know of a relevant reference for EHT 1864, please let us know.
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Keywords: EHT 1864, EHT 1864 supplier, Rac-GEF, interaction, antioncogenic, G, Proteins, Small, transformation, Rac1, Rac1b, Rac2, Rac3, Ras, Tiam, inhibits, inhibitors, GTPases, EHT1864, Rho, 3872, Tocris Bioscience
19 Citations for EHT 1864
Citations are publications that use Tocris products. Selected citations for EHT 1864 include:
Lionarons et al (2019) RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance. Cancer Cell 36 68 PMID: 31257073
Bridgewater et al (2017) Extracellular matrix promotes clathrin-dependent endocytosis of prolactin and STAT5 activation in differentiating mammary epithelial cells. Sci Rep 7 4572 PMID: 28676702
Xiang et al (2016) 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. J Biol Chem 291 6912 PMID: 26867574
Chung et al (2015) Albumin-associated free fatty acids induce macropinocytosis in podocytes. J Clin Invest 125 2307 PMID: 25915582
Goka and Lippman (2015) Loss of the E3 ubiquitin ligase HACE1 results in enhanced Rac1 signaling contributing to breast cancer progression. Am J Physiol Lung Cell Mol Physiol 34 5395 PMID: 25659579
Mishima and Sharma (2011) Tannerella forsythia invasion in oral epithelial cells requires phosphoinositide 3-kinase activation and clathrin-mediated endocytosis. Arthritis Rheum 157 2382 PMID: 21622527
Dillon et al (2015) P-REX1 creates a positive feedback loop to activate growth factor receptor, PI3K/AKT and MEK/ERK signaling in breast cancer. Oncogene 34 3968 PMID: 25284585
Wang et al (2015) Inhibition of prostate smooth muscle contraction and prostate stromal cell growth by the inhibitors of Rac, NSC23766 and EHT1864. Br J Pharmacol 172 2905 PMID: 25631101
Gadepalli et al (2013) Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration. Oncogene 288 30815 PMID: 24025335
Dipaolo et al (2013) Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells. Microbiology 305 L141 PMID: 23686855
Long et al (2013) Rac1 is required for matrix metalloproteinase 13 production by chondrocytes in response to fibronectin fragments. Cell Cycle 65 1561 PMID: 23460186
Kruppa et al (2018) Myosin VI-Dependent Actin Cages Encapsulate Parkin-Positive Damaged Mitochondria. Dev Cell 44 484 PMID: 29398621
Dendo et al (2018) Induction of non-apoptotic programmed cell death by oncogenic RAS in human epithelial cells and its suppression by MYC overexpression. Carcinogenesis 39 202 PMID: 29106503
Ford et al (2018) Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry. PLoS Pathog 14 e1007051 PMID: 29727463
Zhang et al (2013) The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval. J Neurosci 33 5006 PMID: 23486971
Nagase et al (2016) Deletion of Rac1GTPase in the Myeloid Lineage Protects against Inflammation-Mediated Kidney Injury in Mice. PLoS One 11 e0150886 PMID: 26939003
Goodnough et al (2012) Inhibition of hepcidin transcription by growth factors. Hepatology 56 291 PMID: 22278715
Katz et al (2012) Targeting of Rac GTPases blocks the spread of intact human breast cancer. Oncotarget 3 608 PMID: 22689141
Li et al (2016) Unravelling the Mechanism of TrkA-Induced Cell Death by Macropinocytosis in Medulloblastoma Daoy Cells. Mol.Cell Biol. 36 2596 PMID: 27503856
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Reviews for EHT 1864
Average Rating: 3 (Based on 1 Review.)
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Used to block Rac but no effect seen. Can't say if the compound actually works or not.
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