In vitro
As an ATP-competitive inhibitor, WYE-125132 can potently inibit mTOR with IC50 of 0.19 nM. And WYE-125132 shows >5,000-fold selective versus PI3Ks. WYE-132 also can inhibit mTORC1 and mTORC2. WYE-132 targeted P-AKT(S473) and AKT function without significantly reducing the steady-state level of P-AKT(T308), which is the PI3K/PDK1 activity biomarker. WYE-132 shows stronger inhibition of cancer cells than that of temsirolimus. WYE-132 can inhibit cell growth and survival, protein synthesis, cell size, bioenergetic metabolism, and adaptation to hypoxia. Treatment of cancer cells with WYE-132 leads to a rapid loss of the phosphorylation at Ser-75. WYE-132-induced Maf1 dephosphorylation correlated with its accumulation in the nucleus and a marked decline in the cellular levels of pre-tRNAs.
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