mtor kinase

can be used in research in the fields of chemistry and life sciences.

2H-Imidazo[4,5-b]pyrazin-2-one, 1,3-dihydro-6-[6-(1-hydroxy-1-methylethyl)-3-pyridinyl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- is a potent mTOR inhibitor with IC50 of 0.176 μM and >30 μM for mTOR and PI3Kα, respectively.

Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3 7 7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

3CAI is a potent and specific AKT1 and AKT2 inhibitor, demonstrating significant inhibition of AKT in an in vitro kinase assay. It suppressed the expression of AKT direct downstream targets (such as mTOR and GSK3β) and induced growth inhibition and apoptosis in colon cancer cells.

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.

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.

PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor, with Ki values of 0.13 nM and 1.42 nM, respectively.

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Dactolisib Tosylate (BEZ235 Tosylate) is a dual kinase inhibitor targeting PI3K and mTOR, with IC50 values of 4, 75, 7, and 5 nM for PI3Kα, β, γ, and δ, respectively. It also inhibits mTORC1 and mTORC2.

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

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.

KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.

Cyclovirobuxine D (Bebuxine) is extracted from Buxus microphylla.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM ATR DNA-PK inhibition is 28 nM 35 nM 118 nM, respectively.

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

Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K Akt signaling pathway.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase AKT mTOR pathway and delays sensitive cells in late mitosis.

Insecticidal agent 364 is a selective small molecule inhibitor of rapamycin kinase target protein. Insecticidal agent 364 has antitumor activity, and by inhibiting mTOR, Insecticidal agent 364 aims to disrupt signaling pathways involved in cancer cell growth and survival, thereby potentially inhibiting tumor growth.

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).