p-mtor

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

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.

Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1 P-S6K(T389) and mTORC2 P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

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

Palomid 529 (SG 00529) has been used in trials studying the treatment of Age-Related Macular Degeneration.

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

AV457 is a potent and selective inhibitor of mTOR. It effectively suppresses cyst growth in polycystic kidney disease (PKD) organoids. AV457 reduces the protein expression of P-s6 and P-p70s6, but it does not decrease the protein expression of P-AKT.

ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor with an IC50 of 1135 nM. It demonstrates excellent antiproliferative activity against lung cancer cells H2228, with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation at the G0/G1 phase by affecting mitochondrial function. It exhibits antitumor effects by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. This compound is applicable for research into non-small cell lung cancer (NSCLC).

P-2281 is an mTOR inhibitor with anticancer and anti-inflammatory properties.P-2281 inhibits dextran sulfate sodium (DSS)-induced colitis by suppressing T-cell function and is effective in a mouse model of human colitis.

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

RMC-4529 is a chemical compound that demonstrates potent inhibition, with an IC50 value of 1.0 nM, against p-4E-BP1-(T37/46) in mTOR kinase cellular assays.

(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.

WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2 P-AKT(S473) and mTORC1 P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

WYE-687 is an ATP-competitive and selective inhibitor of mTOR with an IC50 of 7 nM; it blocks mTORC1 pS6K(T389) and mTORC2 P-AKT(S473) without affecting P-AKT(T308). Its selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

PABA NO is a novel glutathione-S-transferase-p-activated nitric oxide donor, inhibiting proliferation and inducing apoptosis by targeting PI3K AKT mTOR and MEK ERK pathways in hepatocellular carcinoma cells.

Indium (III) thiosemicarbazone 5b is an anticancer compound demonstrating cytotoxicity against various cancer cell lines including A549, MCF-7 breast, cisplatin-resistant MCF-7/DDP breast, and Hl 7702 liver cancer cells, with IC50 values of 2.41, 1.97, 2.11, and 8.95 µM, respectively. It effectively lowers PI3K, Akt, mTOR, P-gp, and GSH levels in MCF-7/DDP cells. In vivo studies show that at a dosage of 2.5 µmol/kg, indium (III) thiosemicarbazone 5b significantly reduces tumor weight and volume in MCF-7/DDP mouse xenograft models. Furthermore, liposomes formulated with this compound promote apoptosis and pro-death autophagy in MCF-7/DDP cells, alongside notable reductions in tumor volume and weight, showcasing its potential as a therapeutic agent in cancer treatment.

MD102, with an IC50 value of 0.35 μM, is a potent TG2 inhibitor that stabilizes p53 by inhibiting TG2. This results in a decrease in p-AKT and p-mTOR downstream signaling, ultimately inducing tumor cell apoptosis [1].

WRX606 is an inhibitor of the mammalian target of rapamycin complex 1 (mTORC1). In MCF-7 cells, it inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (p-S6K1) with an IC50 value of 10 nM, and the phosphorylation of eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) with an IC50 of 0.27 μM. Additionally, WRX606 exhibits cytotoxicity in HepG2 cells with an IC50 of 17 nM and has demonstrated antitumor efficacy in mouse models.