fti277

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

FTI-277 hydrochloride is a farnesyl transferase inhibitor and highly potent Ras CAAX peptidomimetic that antagonizes both H-Ras and K-Ras oncogenic signaling pathways, FTI-277 hydrochloride additionally inhibits hepatitis delta virus infection, making it a valuable compound for studying Ras-driven oncogenesis, protein prenylation, and antiviral intervention strategies.

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.