EHT 1864

754240-09-0

C25H29Cl2F3N2O4S

DMSO : >= 32 mg/mL (55.03 mM); H2O : >= 100 mg/mL (171.97 mM)

GPCR/G Protein

EHT 1864 is a small molecule inhibitor of Rac1 signaling; modulate gamma-Secretase-mediated APP processing. IC50 value: Target: Rac1 inhibitor in vitro: EHT 1864 blocks Abeta 40 and Abeta 42 production but does not impact sAPPalpha levels and does not inhibit gamma-secretase. Rather, EHT 1864 modulates APP processing at the level of gamma-secretase to prevent Abeta40 and Abeta42 generation. This effect does not result from a direct inhibition of the gamma-secretase activity and is specific for APP cleavage, since EHT 1864 does not affect Notch cleavage [1]. EHT 1864 specifically inhibited Rac1-dependent platelet-derived growth factor-induced lamellipodia formation. Furthermore, our biochemical analyses with recombinant Rac proteins found that EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms, and this association promoted the loss of bound nucleotide, inhibiting both guanine nucleotide association and Tiam1 Rac guanine nucleotide exchange factor-stimulated exchange factor activity in vitro [2]. in vivo: EHT1864 significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains at a threshold that is compatible with delaying plaque accumulation and/or clearing the existing plaque in brain [1].