fti 276 tfa

FTI 276 TFA is effective against plasmodium falciparum and humans.It is a protein-based nikyltransferase (PFT) inhibitor with an IC50s of 0.9 nM and 0.5 nM, respectively.

FTI 277 TFA is a prodrug form of FTI 276 that inhibits farnesyltransferase (FTase) (IC50 = 0.5 nM). Inhibits H-Ras and K-Ras processing in whole cells (IC50 values are 0.1 and 10μM respectively) and disrupts constitutive H-Ras-specific activation of MAPK. Causes significant antiproliferative effects in human malignant glioma cells and many other tumor cell lines.

FTI-2153 TFA is a highly selective and potent inhibitor of the farnesyltransferase (FTase) enzyme (IC50: 1.4 nM). The inhibition activity was more than 3000 times that of Rap1A protein processing.

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

GGTI-286 TFA is a potent, cell-permeable inhibitor of GGTase I, exhibiting 25 times greater effectiveness (IC 50 = 2 μM) compared to the corresponding methyl ester of FTI-276. It specifically targets the geranylgeranylation of Rap1A, demonstrating significant selectivity over the farnesylation of H-Ras in NIH3T3 cells (IC 50s = 2 and >30 μM, respectively). Additionally, GGTI-286 TFA effectively inhibits the stimulation of oncogenic K-Ras4B with an IC 50 of 1 μM.