RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.
YB-3−17 is a dual-target compound that effectively and selectively inhibits mTOR with an IC50 of 0.22 nM, while promoting GSPT1 degradation with an IC50 of 5 nM, leading to substantial tumor growth inhibition both in vitro and in vivo. It also exhibits significant antiproliferative activity in glioblastoma models.
PD-M6 is an mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes the ubiquitination and degradation of mTOR. PD-M6 inhibits the proliferation of HeLa, MCF-7, and HepG2 cancer cell lines (IC50 values of 11.3, 2.58, and 3.23 μM, respectively) and induces autophagy. PD-M6 specifically induces the degradation of LAMTOR1, a key protein in the mTOR signaling pathway.
AV457 is a potent and selective mTOR inhibitor with an IC50 value of 0.54 µM. AV457 inhibits cyst growth in polycystic kidney disease (PKD) organoids. AV457 decreases the protein expression of P-s6, P-p70s6 and don’t decreases the protein expression of P-AKT.
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