WYE125132 is an orally-available, ATP-competitive, pyrazolopyrimidine-based, specific inhibitor of mTORC1 and mTORC2 with an mTOR potency of 0.19 nM and >5000-fold selectivity against the PI3K isoform family, hSMG1, and ATR enzymes. WYE125132 selectively inhibits phosphorylation of p-Akt (S473) and Akt without significantly reducing levels of T308. FACS analysis reveals that WYE125132 induces cell cycle arrest at the G1-phase, with a reduction in S-phase cells. [1]

WYE125132 induces the rapid loss of phosphorylation at Ser75. Maf1 dephosphorylation was also observed and correlated with its accumulation in the nucleus and a marked decline in the cellular levels of pre-tRNAs. [2]

WYE125132 is an orally-available, ATP-competitive, pyrazolopyrimidine-based, specific inhibitor of mTORC1 and mTORC2 with an mTOR potency of 0.19 nM and >5000-fold selectivity against the PI3K isoform family, hSMG1, and ATR enzymes. WYE125132 selectively inhibits phosphorylation of p-Akt (S473) and Akt without significantly reducing levels of T308. FACS analysis reveals that WYE125132 induces cell cycle arrest at the G1-phase, with a reduction in S-phase cells. [1]

WYE125132 induces the rapid loss of phosphorylation at Ser75. Maf1 dephosphorylation was also observed and correlated with its accumulation in the nucleus and a marked decline in the cellular levels of pre-tRNAs. [2]