EHT 1864

EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG[1][2][3][4].

Product Specifications

CAS Number

[754240-09-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ras

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/EHT-1864.html

Purity

99.85

Solubility

DMSO : ≥ 32 mg/mL|H2O : ≥ 100 mg/mL

Smiles

O=C1C=C(CN2CCOCC2)OC=C1OCCCCCSC3=CC=NC4=CC(C(F)(F)F)=CC=C34.[H]Cl.[H]Cl

Molecular Formula

C25H29Cl2F3N2O4S

Molecular Weight

581.48

Precautions

H302, H315, H319, H335

References & Citations

[1]Desire L, et al. RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo. J Biol Chem. 2005 Nov 11;280 (45) :37516-25.|[2]Shutes A, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. J Biol Chem. 2007 Dec 7;282 (49) :35666-78.|[3]Onesto C, et al. Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 2008;439:111-29.|[4]Ying Liu , et al. Podocyte-Released Migrasomes in Urine Serve as an Indicator for Early Podocyte Injury. Kidney Dis (Basel) . 2020 Nov;6 (6) :422-433.