mtor (p70s6k)

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.

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.

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).

Hu7691 free base is an orally active, potent, and selective Akt inhibitor with anti-proliferative and neurogenic effects on various neuroblastoma cell lines. It inhibits Akt1, Akt2, and Akt3, and induces differentiation of neuroblastoma cells.

Chrysophanol (Turkey Rhubarb) is an EGFR mTOR pathway inhibitor, which can be found in rhubarb, and sorrel.

3'-Hydroxypterostilbene (3'-HPT), a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells with IC50s of 9.0, 40.2, and 70.9 μM for COLO 205, HCT-116, and HT-29 cells, respectively, by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the p38MAPK , and PI3K Akt mTOR p70S6K pathways and activates the ERK1 2, JNK1 2 MAPK pathways[1].

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

AT-533 is a potent inhibitor of Hsp90 and HSV. AT-533 blocks the HIF-1α VEGF VEGFR-2 signaling pathway, leading to suppress tumor growth and angiogenesis. AT-533 also inhibits the activation of the downstream pathways, including Erk1 2, FAK, Akt mTOR p70S6K,. AT-533 inhibits the cell migration, invasion, and the tube formation of human umbilical vein endothelial cells (HUVECs).

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

(32-Carbonyl)-RMC-5552 is a highly effective mTOR inhibitor, inhibiting both mTORC1 and mTORC2 substrate phosphorylation. It significantly suppresses the phosphorylation of p-P70S6K-(T389), p-4E-BP1-(T37 36), and p-AKT1 2 3-(S473) with pIC50 values >9, >9, and 8~9, respectively.

AMPK activator 2 is a chloroformin derivative with potential anticancer activity, which can up-regulate AMPK signaling pathway and down-regulate mTOR 4EBP1 p70S6K, and inhibit proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

AMPK activator 2 hydrochloride is a fluoroguanidine-containing derivative that up-regulates the AMPK signaling pathway and down-regulates mTOR 4EBP1 p70S6K.AMPK activator 2 hydrochloride inhibits the proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).

22-(4′-py)-JA, a semisynthetic derivative of junamycin A isolated from the Thai blue sponge (Xestospongia sp.), exhibits antimetastatic properties by inhibiting the AKT mTOR p70S6K signaling pathway. It also impedes tumor cell invasion and angiogenesis in human umbilical vein endothelial cells (HUVEC), while suppressing the expression of metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer activity is particularly noted against non-small cell lung cancer (NSCLC) [1].

Mito-LND (Mito-Loidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation.

Zederone is a natural sesquiterpene that modulates inflammatory response, smooth muscle relaxation and endocrinology to treat dysmenorrhea; down-regulates mRNA levels of mTOR and p70s6K to inhibit the proliferation of ovarian cancer cells, and interacts with hypoglycemic proteins 3L4Y and 5UBA to be anti-diabetic and anti-oxidant.