EHT 1864 2HCl
Molecular Weight(MW): 581.47
EHT 1864 2HCl 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.
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E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
FASEB J, 2018, 32(4):2197-2211. EHT 1864 2HCl purchased from Selleck.
Inhibition of Rac1 activity by EHT 1864 blocks alignment under flow, whereas solvent control-treated ECs aligned in the direction of flow. Note that the inhibitor was present throughout the experiment, due to the closed system that is used for long-term flow experiments. Bar graph on the right shows percentage of aligned cells in under static and flow conditions for both EHT 1864-treated and solvent-treated Ctrl ECs. ECs orientated between a 0-45° angle are quantified as being aligned. Data are mean of three independent experiments ± SEM. ***P<0.001. Bar, 25μm.
Mol Biol Cell, 2017, 28(13):1745-1753. EHT 1864 2HCl purchased from Selleck.
EHT1864 influences the expression of Rac1 and upregulates ILC2 associated cytokines. In order to further prove the role of Rac1 in the occurrence of asthma, the mice were treated by EHT1864 before allergen provoking, it resulted in more enhanced expression levels of ILC2s related cytokines along with decreased expression level of Rac1 in asthmatic mice. (A) The expression level of Rac1 mRNA in the lung tissue; (B) The expression level of Rac1 mRNA in PBMC; (C) The expression level of IL-33 mRNA in the lung tissue; (D) IL-33 protein levels in BALF detected by ELISA; (E) IL-33 protein levels in plasma detected by ELISA. The results of immunofluorescence assay showed that the Rac1 expression in the bronchial from control group (F), asthma group (G) and asthma+EHT1864 group (H). In addition, the results of H&E staining showed that the inflammatory was aggravated in asthma mice and asthma+EHT1864 group. (I) The pathological changes (×200) in lung tissue from control group; (J) The pathological changes (×200) in lung tissue from asthmatic group; (K) The pathological changes (×200) in lung tissue from EHT1864 inhibited group. Data shown are represented as mean ± SD (all samples were measured in triplicate). *P < 0.05, **P < 0.01, ***P < 0.001.
Int J Clin Exp Pathol, 2016, 9(6):5902-5911.. EHT 1864 2HCl purchased from Selleck.
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|Description||EHT 1864 2HCl 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.|
EHT 1864 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. 
|In vivo||EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. |
Inhibitor:GTPase binding analyses:For inhibitor:GTPase binding analyses, aliquots of small GTPase solution (containing 1 μM inhibitor) are titrated into a solution of 1 μM inhibitor in the cuvette. Changes in fluorescence anisotropy are monitored at λex = 360 nm, λem = 440 nm, 30 s after each addition. All data analysis and curve fitting were performed using Microsoft Excel and QuantumSoft's ProFit for Mac OS X.
|In vitro||DMSO||100 mg/mL warmed (171.97 mM)|
|Water||100 mg/mL (171.97 mM)|
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