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EHT1864

Chemical Structure : EHT1864

CAS No.: 754240-09-0

EHT1864 (EHT 1864)

Catalog No.: PC-49212Not For Human Use, Lab Use Only.

EHT1864 is a small molecule Rac inhibitor that blocks the Rac1 signaling pathways with IC50 of 5 uM in cellular luciferase assays, binds to Rac1b and Rac2 with very similar affinities (50 and 60 nM, respectively).

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Biological Activity

EHT1864 is a small molecule Rac inhibitor that blocks the Rac1 signaling pathways with IC50 of 5 uM in cellular luciferase assays, binds to Rac1b and Rac2 with very similar affinities (50 and 60 nM, respectively).
EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms, interferes with the process of nucleotide exchange on Rac1.
EHT 1864 specifically inhibited Rac1-dependent platelet-derived growth factor-induced lamellipodia formation.
EHT 1864 reduces production of Aβ 40 and 42 amyloid peptides in SH-SY5Y cells endogenously expressing wild type APP with IC50 of 5.4 uM, does not affect α-secretase and BACE pathways.
EHT 1864 (40 mg/kg/day, oral) reduces Aβ 40 levels in adult albino guinea pig brain.

Physicochemical Properties

M.Wt 581.472
Formula C25H29Cl2F3N2O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(5-(7-(trifluoromethyl)quinolin-4-ylthio)pentyloxy)-2-(morpholinomethyl)-4H-pyran-4-one dihydrochloride

References

1. Bhanot H, et al. J Biol Chem. 2005 Nov 11;280(45):37516-25.

2. Shutes A, et al. J Biol Chem. 2007 Dec 7;282(49):35666-78.

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