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EHT 1864

Catalog No. T6483 CAS 754240-09-0

Synonyms: EHT 1864 2HCl

EHT 1864 is a effective Rac family GTPase inhibitor for Rac1/Rac1b/Rac2/Rac3 (Kd: 40/50/60/250 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

EHT 1864, CAS 754240-09-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 84.00
10 mg	In stock	$ 138.00
25 mg	In stock	$ 273.00
50 mg	In stock	$ 497.00
100 mg	In stock	$ 712.00
200 mg	In stock	$ 983.00
1 mL * 10 mM (in DMSO)	In stock	$ 109.00

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Purity: 99.42%

Purity: 99.18%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EHT 1864 is a effective Rac family GTPase inhibitor for Rac1/Rac1b/Rac2/Rac3 (Kd: 40/50/60/250 nM).
Targets&IC50	Rac2:60 nM(Kd), Rac1b:50 nM(Kd), Rac3:250 nM(Kd), Rac1:40 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]
In vivo	EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. [2]
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	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)

Synonyms	EHT 1864 2HCl
Molecular Weight	581.47
Formula	C25H29Cl2F3N2O4S
CAS No.	754240-09-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (85.99 mM)

H2O: 58.2 mg/mL (100 mM)

References and Literature

1. Shutes A, et al. J Biol Chem. 2007, 282(49), 35666-35678. 2. Désiré L, et al. J Biol Chem. 2005, 280(45), 37516-3752 3. Raynaud F, et al. J Biol Chem. 2014, 289(5), 2600-2609. 4. Liu X, Wang S, Zheng H, et al. Epimedokoreanin C, A Prenylated Flavonoid Isolated from Epimedium Koreanum, Induces Non-Apoptotic Cell Death with the Characteristics of Methuosis in Lung Cancer Cells[J]. 2020

Citations

1. Weddle E A, Köseoğlu V K, DeVasure B A, et al. The type three secretion system effector protein IpgB1 promotes Shigella flexneri cell-to-cell spread through double-membrane vacuole escape. PLoS Pathogens. 2022, 18(2): e1010380 2. Liu X, Wang S, Zheng H, et al. Epimedokoreanin C, A Prenylated Flavonoid Isolated from Epimedium Koreanum, Induces Non-Apoptotic Cell Death with the Characteristics of Methuosis in Lung Cancer Cells. American Journal of Cancer Research. 2021, 11(7): 3496. 3. Liu Y, Sun Y, Xu Y, et al.Targeting VPS41 induces methuosis and inhibits autophagy in cancer cells.Cell Chemical Biology.2023

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library MAPK Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Alzheimer's Disease Compound Library Anti-COVID-19 Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EHT 1864 754240-09-0 Cell Cycle/Checkpoint GPCR/G Protein MAPK Ras Rho EHT 1864 2HCl precursor β-amyloid protein disease Alzheimer amyloid EHT1864 inhibit transformation Inhibitor EHT-1864 inhibitor

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