EHT 1864

EHT 1864 is a potent, small molecule inhibitor of the Rac family of small GTPases, specifically targeting Rac1, Rac1b, Rac2, and Rac3. It employs a unique mechanism of action by binding to Rac proteins with high affinity and inducing the displacement of guanine nucleotides (GDP and GTP). This action locks the Rac proteins in an inert, inactive state, effectively preventing their interaction with downstream signaling effectors. Developed by ExonHit Therapeutics, EHT 1864 is widely utilized as a pharmacological research tool to study Rac-dependent cellular processes, including actin cytoskeleton remodeling (lamellipodia formation), cell proliferation, and oncogenic transformation. It has been investigated for its potential therapeutic applications in reducing β-amyloid peptide production in Alzheimer's disease and inhibiting growth in cancer cells. Additionally, research has highlighted its role in rescuing phenotypes associated with KCNA2 variants, such as dilated cardiomyopathy, obesity, and sleep apnea, by modulating the RAC-ERK pathway.

Other names

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