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.

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).

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.

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

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.

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50 values of 38.69, 40.12, and 59.72 nM, respectively. It also serves as an autophagy agonist, influencing mTOR/p70S6K and NCOA4-mediated ferroptosis, potentially mitigating multidrug resistance. SKLB-D18 demonstrates significantly superior efficacy against triple-negative breast cancer (TNBC) in both in vitro and in vivo studies.

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).

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).

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].

2-APQC is a selective, orally active Sirtuin-3 (SIRT3) agonist (Kd=2.756 μM) that modulates mitochondrial homeostasis. It attenuates ISO-induced myocardial hypertrophy and fibrosis in vivo and in vitro, making it suitable for heart failure research. 2-APQC inhibits mTOR-p70S6K, JNK, TGF-β/Smad3, and ROS-p38MAPK pathways while activating PYCR1 and AMPK-Parkin, thereby suppressing necrosis and mitigating mitochondrial oxidative damage.

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.