mtor inhibitor 8

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.

PI3K/mTOR Inhibitor-8 is a dual inhibitor of PI3K (PI3Kα IC50: 0.46 nM) and mTOR (mTOR IC50: 12 nM). PI3K/mTOR Inhibitor-8 blocks the cell cycle of HCT-116 cells in G1/S phase and induces apoptosis. apoptosis).

mTOR inhibitor 9a inhibited the growth of human LNCap cells with an ic50 of 80 nm. 1-methyl-3 -{4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl}urea may have antitumor activity.

mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.

AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.

YY2201 is a potent, selective inhibitor of ATR with an IC50 of 8 nM. It exhibits over 200 times greater selectivity for ATR compared to mTOR. Additionally, YY2201 is capable of inhibiting tumor progression across a wide range of cancer types.

PI3K/mTOR-IN-17 is a dual inhibitor that targets both PI3K and mTOR, with IC50 values of 1.21 μM and 0.21 μM, respectively. It induces apoptosis mediated by caspases and arrests cell growth in the G1 phase. The compound elevates the levels of caspases-3, 7, 8, and 9, enhances p53 expression, and increases the Bax/Bcl-2 ratio. By inhibiting the PI3K/mTOR signaling pathway, PI3K/mTOR-IN-17 is applicable in cancer research, including studies on non-small cell lung cancer (NSCLC).

Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).

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).

PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

Cobaltic Protoporphyrin IX chloride (CoPP) is a potent heme oxygenase 1 (HO-1) inducer with antiviral activity that inhibits influenza A virus (IAV) infection by inducing a type I IFN response. mTOR inhibitor-8 is a potent mTOR inhibitor and autophagy inducer with antiviral and antitumor activities.

(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.

DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).

PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor exhibiting nM-level inhibition of p110α, p110β, p110δ, p110γ, DNA-PK, mTORC1, and mTORC2. PI-103 induces autophagy, mitochondrial apoptosis, and cell cycle arrest, making it suitable for leukaemia research.

PI3K-IN-37 (Example 84.1) is an inhibitor of PI3K α (IC50: 6 nM), PI3K β (IC50: 8 nM), and PI3K δ (IC50: 4 nM), and also inhibits mTOR with an IC50 of 4 nM.

PI3Kα-IN-21 (compound 8) is a selective inhibitor of PI3Kα, demonstrating greater selectivity over PI3Kβ, PI3Kγ, and PI3Kδ by factors of 10.41, 16.99, and 37.53 respectively (IC50: 96.89/568.24/397.48 nM). This compound inhibits cancer cell activity, proliferation, and migration while inducing mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. Additionally, PI3Kα-IN-21 has shown in vivo antitumor efficacy in a mouse model of non-small cell lung cancer.

Lupiwighteone has anti-angiogenesis potential, it also has anticancer and cancer preventive effects on SH-SY5Y cells.