target/mTOR/5

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

YB-3-17 is a bifunctional molecule that can inhibit mTOR with an IC50 of 0.22 nM or degrade the G1 to S phase transition 1 gene (GSPT1) through the PROTAC mechanism, with a DC50 of 5 nM. It exhibits antiproliferative activity at nanomolar concentrations in various glioblastoma cell lines. Additionally, YB-3-17 shows antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase Cereblon)

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K mTOR. Activation of the PI3K mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

PKI-179 is a potent, orally active compound that functions as a dual PI3K mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PQR626 is a rapamycin derivative that acts as a highly potent, selective, orally active, and brain-penetrant mTOR inhibitor. It exhibits remarkable inhibitory effects on the mammalian target of the rapamycin (mTOR) pathway, with an IC50 value of 5 nM and a Ki value of 3.6 nM. This compound, PQR626, holds promise for advancing research in the field of neurological disorders.