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EHT 1864

Catalog No.GC10660

Rac family small GTPases inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

EHT 1864 Chemical Structure

Cas No.: 754240-09-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$78.00
In stock
10mg
$93.00
In stock
50mg
$415.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

INS-1 832/13 cells (Insulin-Producing-Cell Line)

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1 h

Applications

10 μM EHT 1864 shows a complete inhibition of GSIS (Glucose-stimulated insulin secretion)and inhibits GSIS at 10-20mM glucose. It also suppresses a glucose-induced membrane association of Rac1 and glucose-induced ERK1/2 phosphorylation and activation.

References:

1. Sidarala V, Veluthakal R, Syeda K, Kowluru A. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells. Cell Signal. 2015 Jun;27(6):1159-67.

Background

EHT 1864 is a small-molecule inhibitor of Rac family small GTPases with Kd value of 40nM for Rac1 [1].

In NIH 3T3 mouse fibroblasts, EHT 1864 treatment shows an 80% reduction in PDGF-induced lamellipodia formation. EHT 1864 at concentration of 50μM can completely inhibit the complex formation between Rac1 and PAK-RBD and cause the release of nucleotide from Rac1. The reassociation of nucleotide with Rac1 induced by EDTA or the Tiam1 can also be blocked by EHT 1864. EHT 1864 is most potent to Rac1, both in the binding affinity and stimulation of nucleotide release. It binds to Rac1b, Rac2 and Rac3 with Kd values of 50nM, 60nM and 250nM, respectively. Moreover, EHT 1864 can suppress cellular transformation induced by Rac1 with an 80% inhibition of focus-forming activity [1].

References:
[1] Shutes A, Onesto C, Picard V, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Journal of Biological Chemistry, 2007, 282(49): 35666-35678.

Chemical Properties

Cas No. 754240-09-0 SDF
Canonical SMILES FC(F)(C1=CC=C2C(SCCCCCOC3=COC(CN4CCOCC4)=CC3=O)=CC=NC2=C1)F.Cl.Cl
Formula C25H29Cl2F3N2O4S M.Wt 581.48
Solubility ≥ 29.05mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.7197 mL 8.5987 mL 17.1975 mL
5 mM 0.3439 mL 1.7197 mL 3.4395 mL
10 mM 0.172 mL 0.8599 mL 1.7197 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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