EHT 1864

Name: EHT 1864
Brand: Tocris Bioscience
SKU: 3872
Rating: 3 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 3872

(1)

Citations (101)

COA / SDS

Potent Rac family inhibitor

Key Product Details

Description:	Potent Rac family inhibitor
Chemical Name:	5-(5-(7-(Trifluoromethyl)quinolin-4-ylthio)pentyloxy)-2-(morpholinomethyl)-4H-pyran-4-one dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	581.47

View Full Technical Details for EHT 1864

Technical Data
Citations / Reviews (1)

Biological Activity for EHT 1864

EHT 1864 is an inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (K_D values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo.

Licensing Information

Sold for research use only under license from ExonHit Therapeutics S.A.

Compound Libraries for EHT 1864

EHT 1864 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for EHT 1864

M. Wt	581.47
Formula	C₂₅H₂₇F₃N₂O₄S.2HCl
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	754240-09-0
PubChem ID	9938202
InChi Key	LSECOAJFCKFQJG-UHFFFAOYSA-N
Smiles	O=C1C=C(CN4CCOCC4)OC=C1OCCCCCSC3=CC=NC2=CC(C(F)(F)F)=CC=C23.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for EHT 1864

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	11.63	20
	DMSO	43.61	75

Preparing Stock Solutions for EHT 1864

The following data is based on the product molecular weight 581.47.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.75 mM	2.29 mL	11.47 mL	22.93 mL
3.75 mM	0.46 mL	2.29 mL	4.59 mL
7.5 mM	0.23 mL	1.15 mL	2.29 mL
37.5 mM	0.05 mL	0.23 mL	0.46 mL

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References for EHT 1864

References are publications that support the biological activity of the product.

Shutes Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases. J.Biol.Chem. 2007 PMID: 17932039
Onesto Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 2008 PMID: 18374160
Desire RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo. J.Biol.Chem. 2005 PMID: 16150730