at 2153

FTI-2153 is a potent and highly selective farnesyltransferase (FTase) inhibitor (IC50: 1.4 nM) that is over 3000-fold more effective at blocking H-Ras (IC50: 10 nM) than Rap1A processing.

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.

TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), exhibiting psychotropic activity and low acute toxicity. It enhances the expression of brain-derived neurotropic factor (BDNF) in the brain, reduces mRNA levels of MAOA and 5-HT1A receptors in the midbrain, and inhibits 5-HT2A receptor-mediated signaling.

Probimane (AT-2153) had Anti-proliferative effects, cell cycle G2/M phase arrest and blocking of chromosome segregation in human tumor cell lines with MST-16.