mTOR

Rapamycin (Sirolimus) is a macrolide mTOR inhibitor (IC 50 =0.1nM).

MTORC1 and mTORC2 inhibitor

Pan-PI3K/mTOR inhibitor

PF-05212384 (PKI-587) is a potent dual PI3K/mTOR inhibitor, exhibiting inhibitory effects against PI3Kα (IC₅₀=0.4nM), PI3Kβ (IC₅₀=6nM), PI3Kγ (IC₅₀=8nM), PI3Kδ (IC₅₀=6nM), and mTOR (IC₅₀=1.4nM).

mTORC1 and mTORC2 inhibitor

PP242 (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively.

BGT226 (NVP-NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

PI-103 Hydrochloride is a potent cell-permeable multi-target inhibitor that primarily acts on the PI3K and mTOR signaling pathways.

AZD8055 is a new ATP-competitive mTOR inhibitor with an IC 50 of 0.8 nmol/L and a K i of 1.3 nmol/L.

PF-04691502 is an orally active, ATP-competitive dual inhibitor of PI3K and mTOR, with K i values of 1.2, 2.1, 1.6, and 1.9nM for PI3Kα, β, δ, and γ isoforms, respectively.

An mTOR inhibitor

mTOR/DNA-PK inhibitor

PI3K inhibitor,selective, reversible and ATP-competitive

(+)-Usniacin is isolated from isolated from lichens, binds at the ATP-binding pocket of mTOR, and inhibits mTORC1/2 activity. (+)-Usniacin inhibits the phosphorylation of mTOR downstream effectors: Akt (Ser473), 4EBP1, S6K, induces autophay, with anti-cancer activity. (+)-Usniacin possesses antimicrobial activity against a number of planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium.

potent, brain-penetrant PI3K inhibitor

A selective PI3K/mTOR kinase inhibitor

Nordihydroguaiaretic acid is a potent 5-lipoxygenase (5-LOX) inhibitor with an IC 50 value of 8μM.

D-α-Hydroxyglutaric Acid is a weak competitive antagonist of α‑ketoglutarate (α‑KG) (K i = 10.87mM).

CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07.

PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.

PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33nM, 451nM, 661nM, 708nM and 89nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.

4-Vinylcyclohexene dioxide (VCD), a metabolite of 4-vinylcyclohexene (VCH), is synthesized in industries as an intermediate diluent for epoxy resins and other epoxides.

Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).