EHT 1864 2HCl

Catalog No.S7482

EHT 1864 2HCl Chemical Structure

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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USD 795 In stock
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Cited by 5 Publications

4 Customer Reviews

  • 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.

    HE staining of colonic tissue of acute colitis mice. The histologic score was calculated and analyzed. n=5, **, P<0.01.

    Am J Cancer Res, 2018, 8(1):70-80. 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.

Purity & Quality Control

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Biological Activity

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.
Targets
Rac1 [1]
(Cell-free assay)
Rac1b [1]
(Cell-free assay)
Rac2 [1]
(Cell-free assay)
Rac3 [1]
(Cell-free assay)
40 nM(Kd) 50 nM(Kd) 60 nM(Kd) 250 nM(Kd)
In vitro

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. [1] EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. [2] In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse NIH3T3 cells MX7GeY5kfGmxbjDhd5NigQ>? MVnF[oZm[3Rib36gVoFkOSCkaX7kbY5oKHSxIGLoc2dFUTJiaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NV7HcnZvOTd7M{KwN|k>
mouse NIH3T3 cells NFfseHRHfW6ldHnvckBie3OjeR?= MnHiSYZn\WO2IH;uJHJi[zFiYnnu[Ilv\yC2bzDSbI9ITElzIHnuJI1wfXOnIF7JTFNVOyClZXzsd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MmrPNVc6OzJyM{m=
293T cells NV\oUI1jTnWwY4Tpc44h[XO|YYm= M{\QTGVn\mWldDDvckBT[WNzIHLpcoRqdmdidH:gVohwT0SLMjDlfJBz\XO|ZXSgbY4hOjl|VDDj[YxteyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M3HqZVE4QTN{MEO5

... Click to View More Cell Line Experimental Data

In vivo EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. [2]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: NIH 3T3 cells
  • Concentrations: ~5 μM
  • Incubation Time: 4 days
  • Method: NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Male Hartley albino guinea pigs
  • Formulation: Physiological saline
  • Dosages: 40 mg/kg daily
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (171.97 mM)
Water 100 mg/mL (171.97 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 581.47
Formula

C25H29Cl2F3N2O4S

CAS No. 754240-09-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Rho Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID