Home Cell Cycle Rho inhibitor EHT 1864 2HCl For research use only.

EHT 1864 2HCl

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 2HCl Chemical Structure

EHT 1864 2HCl Chemical Structure

CAS No. 754240-09-0

Purity & Quality Control

EHT 1864 2HCl Related Products

Signaling Pathway

Rho Signaling Pathways

Rho Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NIH3T3 Function assay 5 uM Inhibition of lysophosphatidic acid-induced actin stress fibers formation in mouse NIH3T3 cells at 5 uM 17932039
NIH3T3 Function assay 5 uM Inhibition of bradykinin-induced filopodia formation in mouse NIH3T3 cells at 5 uM 17932039
293T Function assay Effect on Rac1 binding to RhoGDI1 expressed in 293T cells by Western blot analysis 17932039
293T Function assay Effect on Rac1 binding to RhoGDI2 expressed in 293T cells by Western blot analysis 17932039
NIH3T3 Function assay Effect on Rac1 binding to RhoGDI1 in mouse NIH3T3 cells by Western blot analysis 17932039
NIH3T3 Function assay Effect on Rac1 binding to RhoGDI2 in mouse NIH3T3 cells by Western blot analysis 17932039
NIH3T3 Function assay 5 uM 3 to 5 weeks Inhibition of Rac1 61L mutant-induced cellular transformation in mouse NIH3T3 cells at 5 uM after 3 to 5 weeks 17932039
NIH3T3 Function assay 5 uM Inhibition on Tiam1 C1199 mutant-induced focus forming activity in mouse NIH3T3 cells at 5 uM 17932039
NIH3T3 Function assay 5 uM Inhibition of Ras-induced cell growth in H-Ras 61L expressing mouse NIH3T3 cells at 5 uM by MTT assay 17932039
U87MG Function assay Reduction of RhoA-GTPase level in platelet derived growth factor-induced human U87MG cells measured with GST-rhotekin-RBD by pulldown assay 17932039
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Rac1 / Rac2 / Rac3 p-STAT3 / STAT3 / p-Bcl-2 / Bcl-2 / Rac1 29416921
Immunofluorescence iNOS 29416921
In Vivo
In vivo EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. [2]
Animal Research Animal Models Male Hartley albino guinea pigs
Dosages 40 mg/kg daily
Administration i.p.

Chemical Information & Solubility

Molecular Weight 581.47 Formula

C25H29Cl2F3N2O4S
CAS No. 754240-09-0 SDF Download EHT 1864 2HCl SDF
Smiles C1COCCN1CC2=CC(=O)C(=CO2)OCCCCCSC3=C4C=CC(=CC4=NC=C3)C(F)(F)F.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (171.97 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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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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