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.

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).

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

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.

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).

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.

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.

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].

(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.

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.

PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].

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

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).

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.