mtor

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

mTOR inhibitor-8 is a potent mTOR inhibitor and autophagy inducer with antiviral and antitumor activity. mTOR inhibitor-8 inhibits the growth of A549 cells, which can be used to study non-small cell lung cancer.

mTOR inhibitor 9b is an enzyme inhibitor of protein kinase mTOR he phosphatidylinositol 3-kinase PIK3CA with IC50s of 0.76 nm and 1.262 µM, respectively.mTOR inhibitor 9b possesses anticancer activity and can be used to study leukemia, skin, breast, lung and colon cancers.

mTOR inhibitor 9f is a selective mTOR inhibitor with IC50 of 1.25nM and 82nM for mTOR and PI3Kα, respectively.

PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

mTOR inhibitor 9e is a selective mTOR inhibitor with IC50 of 0.68nM and 1359nM for mTOR and PI3Kα, respectively.

mTOR inhibitor 9c is a selective mTOR inhibitor with IC50 of 0.7nM and 825nM for mTOR and PI3Kα, respectively.

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.

Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.

Torin 1 is an effective inhibitor of mTORC1 2 with (IC50: 2 nM 10 nM); has 1000-fold selectivity for mTOR than PI3K.

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

WYE-125132 (WYE-132 (WYE-125132)) is a highly potent, ATP-competitive mTOR inhibitor with IC50 of 0.19 nM; highly selective for mTOR versus PI3Ks or PI3K-related kinases hSMG1 and ATR.

hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1 P-S6K(T389) and mTORC2 P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

(+)-Usnic acid (D-Usnic Acid) is a naturally occurring dibenzofuran derivative found in several lichen species.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.

ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).